MK-4827(Niraparib,MK4827)|PARP inhibitor
Niraparib(MK4827) in stock,price: 500 USD/100mg. MK-4827 is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity.
Product Name: Niraparib(MK4827) hydrochloride |cas: 1038915-64-8 |cat number: DC9862 |Molecule Formular: C19H21ClN4O |MW: 356.85 |purity>98%
Description of MK-4827: MK-4827 is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. MK4827 inhibits PARP activity, enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis. The PARP family of proteins detect and repair single strand DNA breaks by the base-excision repair (BER) pathway. The specific PARP family member target For PARP inhibitor MK4827 is unknown. Check For active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).
For the detailed information about the solubility of MK-4827 in water, the solubility of MK-4827 in DMSO, the solubility of MK-4827 in PBS buffer, the animal experiment（test） of MK-4827, the in vivo,in vitro and clinical trial test of MK-4827, the cell experiment（test） of MK-4827, the IC50, EC50 and Affinity of MK-4827 , please contact DC Chemicals.
For research only, not for human use!
2016年11月7日星期一
BMS-779788(XL652)|LXR agonist
BMS-779788(XL652)|LXR agonist
BMS-779788(XL652) is a novel small-molecule modulator of the Liver X Receptor (LXR), a nuclear hormone receptor implicated in a variety of cardiovascular and metabolic disorders.
Product Name: BMS-779788(XL-652) |cas: 918348-67-1 |cat number: DC9861 |Molecule Formular: C28H29ClN2O3S |MW: 508.15 |purity>98%
BMS-779788, also known as XL-652, EXEL 04286652 and BMS-788, is potent partial LXR agonist with LXRβ selectivity, which has an improved therapeutic window in the cynomolgus monkey compared with a full pan agonist. BMS-779788 induced LXR target genes in blood in vivo with an EC50 = 610 nM, a value similar to its in vitro blood gene induction potency. BMS-779788 was 29- and 12-fold less potent than the full agonist T0901317 in elevating plasma triglyceride and LDL cholesterol, respectively, with similar results for plasma cholesteryl ester transfer protein and apolipoprotein B.
For research and scientific purpose only, not for human use.
BMS-779788(XL652) is a novel small-molecule modulator of the Liver X Receptor (LXR), a nuclear hormone receptor implicated in a variety of cardiovascular and metabolic disorders.
Product Name: BMS-779788(XL-652) |cas: 918348-67-1 |cat number: DC9861 |Molecule Formular: C28H29ClN2O3S |MW: 508.15 |purity>98%
BMS-779788, also known as XL-652, EXEL 04286652 and BMS-788, is potent partial LXR agonist with LXRβ selectivity, which has an improved therapeutic window in the cynomolgus monkey compared with a full pan agonist. BMS-779788 induced LXR target genes in blood in vivo with an EC50 = 610 nM, a value similar to its in vitro blood gene induction potency. BMS-779788 was 29- and 12-fold less potent than the full agonist T0901317 in elevating plasma triglyceride and LDL cholesterol, respectively, with similar results for plasma cholesteryl ester transfer protein and apolipoprotein B.
For research and scientific purpose only, not for human use.
KW-2449|cas 1000669-72-6|DC Chemicals
KW-2449|cas 1000669-72-6|DC Chemicals
KW-2449 Hydrochloride in stock,price: 300 USD/100mg. KW 2449 is a multikinase inhibitor of FLT3, ABL, ABL-T315I, and Aurora kinase.
Product Name: KW-2449 Hydrochloride |cas: 1000669-72-6(free base) |cat number: DC9860 |Molecule Formular: C20H20N4O.HCl |MW: 368.86 |purity>98%
KW 2449 is a multikinase inhibitor of FLT3, ABL, ABL-T315I, and Aurora kinase. KW 2449 displays potent inhibition of growth effects on leukemia cells with FLT3 mutations via inhibition of the FLT3 kinase, resulting in the down-regulation of phosphorylated-FLT3/STAT5, G1 arrest, and apoptosis. KW 2449 induces the reduction of phosphorylated histone H3, G2/M arrest, and apoptosis in FLT3 wild-type human leukemia. KW 2449 contributes to release of the resistance by the simultaneous down-regulation of BCR/ABL and Aurora kinases in imatinib-resistant leukemia. KW 2449 inhibitory activity is not affected by the presence of human plasma protein, such as α1-acid glycoprotein. KW 2449 has potent growth inhibitory activity against various types of leukemia by several mechanisms of action. KW 2449 decreases phosphorylation levels of FLT3 and STAT5 in a dose-dependent manner. KW 2449 is a potent inhibitor of ABL-T315I, which is associated with IM resistance (IC50 of 4 nM). KW-2449 has the potent growth inhibitory activities against not only FLT3/ITD-expressing leukemia cells but also FLT3/KDM-activated and wild-type FLT3-overexpressing leukemia cells. KW 2449 suppresses the phosphorylations of FLT3 (P-FLT3) and its downstream molecule phospho-STAT5 (P-STAT5) in MOLM-13 cells in a dose-dependent manner. KW 2449 can dephosphorylate constitutively active WT-FLT3 kinase but not inhibit the proliferation of leukemia cells if they are not mainly addicted to FLT3 the kinase. KW 2449 mediates cytotoxicity through inhibition of FLT3/ITD. KW 2449 is a direct inhibitor of FLT3 and induces inhibition of its downstream target STAT5. KW 2449 interacts synergistically with HDACIs to induce apoptosis in Ph+ CML cells in a time- and concentration-dependent manner. KW 2449 moderately reduces phosphorylation of histone H3, an indicator of Aurora B activity, in nocodozole-treated K562 cells.
For research and scientific purpose only, not for human use.
KW-2449 Hydrochloride in stock,price: 300 USD/100mg. KW 2449 is a multikinase inhibitor of FLT3, ABL, ABL-T315I, and Aurora kinase.
Product Name: KW-2449 Hydrochloride |cas: 1000669-72-6(free base) |cat number: DC9860 |Molecule Formular: C20H20N4O.HCl |MW: 368.86 |purity>98%
KW 2449 is a multikinase inhibitor of FLT3, ABL, ABL-T315I, and Aurora kinase. KW 2449 displays potent inhibition of growth effects on leukemia cells with FLT3 mutations via inhibition of the FLT3 kinase, resulting in the down-regulation of phosphorylated-FLT3/STAT5, G1 arrest, and apoptosis. KW 2449 induces the reduction of phosphorylated histone H3, G2/M arrest, and apoptosis in FLT3 wild-type human leukemia. KW 2449 contributes to release of the resistance by the simultaneous down-regulation of BCR/ABL and Aurora kinases in imatinib-resistant leukemia. KW 2449 inhibitory activity is not affected by the presence of human plasma protein, such as α1-acid glycoprotein. KW 2449 has potent growth inhibitory activity against various types of leukemia by several mechanisms of action. KW 2449 decreases phosphorylation levels of FLT3 and STAT5 in a dose-dependent manner. KW 2449 is a potent inhibitor of ABL-T315I, which is associated with IM resistance (IC50 of 4 nM). KW-2449 has the potent growth inhibitory activities against not only FLT3/ITD-expressing leukemia cells but also FLT3/KDM-activated and wild-type FLT3-overexpressing leukemia cells. KW 2449 suppresses the phosphorylations of FLT3 (P-FLT3) and its downstream molecule phospho-STAT5 (P-STAT5) in MOLM-13 cells in a dose-dependent manner. KW 2449 can dephosphorylate constitutively active WT-FLT3 kinase but not inhibit the proliferation of leukemia cells if they are not mainly addicted to FLT3 the kinase. KW 2449 mediates cytotoxicity through inhibition of FLT3/ITD. KW 2449 is a direct inhibitor of FLT3 and induces inhibition of its downstream target STAT5. KW 2449 interacts synergistically with HDACIs to induce apoptosis in Ph+ CML cells in a time- and concentration-dependent manner. KW 2449 moderately reduces phosphorylation of histone H3, an indicator of Aurora B activity, in nocodozole-treated K562 cells.
For research and scientific purpose only, not for human use.
GAL021|GAL-021|BKCa-channel blocker
GAL021|GAL-021|BKCa-channel blocker
GAL-021 is a new intravenous BKCa-channel blocker.
Product Name: GAL-021 |cas: 1380341-99-0 |cat number: DC9859 |Molecule Formular: 316.18 |MW: |purity>98%
GAL-021 is a new intravenous BKCa-channel blocker,well tolerated and stimulates ventilation in healthy volunteers. GAL-021 was safe and generally well tolerated with adverse events comparable with placebo except for an infusion site burning sensation. GAL-021 stimulated ventilation at the highest doses suggesting that greater infusion rates may be required for maximum PD effects. GAL-021 had PK characteristics consistent with an acute care medication.
For research and scientific purpose only, not for human use.
GAL-021 is a new intravenous BKCa-channel blocker.
Product Name: GAL-021 |cas: 1380341-99-0 |cat number: DC9859 |Molecule Formular: 316.18 |MW: |purity>98%
GAL-021 is a new intravenous BKCa-channel blocker,well tolerated and stimulates ventilation in healthy volunteers. GAL-021 was safe and generally well tolerated with adverse events comparable with placebo except for an infusion site burning sensation. GAL-021 stimulated ventilation at the highest doses suggesting that greater infusion rates may be required for maximum PD effects. GAL-021 had PK characteristics consistent with an acute care medication.
For research and scientific purpose only, not for human use.
CPI455|CPI-455|KDM5 inhibitor
CPI455|CPI-455|KDM5 inhibitor
CPI-455 is a novel specific KDM5 inhibitor.
Product Name: CPI-455 |cas: 1628208-23-0 |cat number: DC9858 |Molecule Formular: C16H14N4O |MW: 278.31 |purity>98%
Novel specific KDM5 inhibitor, elevating global levels of H3K4 trimethylation (H3K4me3) and decreased the number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted agents.
For research and scientific purpose only, not for human use.
CPI-455 is a novel specific KDM5 inhibitor.
Product Name: CPI-455 |cas: 1628208-23-0 |cat number: DC9858 |Molecule Formular: C16H14N4O |MW: 278.31 |purity>98%
Novel specific KDM5 inhibitor, elevating global levels of H3K4 trimethylation (H3K4me3) and decreased the number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted agents.
For research and scientific purpose only, not for human use.
RG-13022|RG13022|EGFR inhibitor
RG-13022|RG13022|EGFR inhibitor
RG-13022 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 1 µM in HT-22 cells.
Product Name: RG-13022 |cas: 136831-48-6 |cat number: DC9857 |Molecule Formular: C16H14N2O2 |MW: 266.3 |purity>98%
RG-13022 is a Tyrosine kinase tyrphostin. Reports indicate that RG-13022 suppresses epidermal growth factor (EGF)-stimulated cancer cell proliferation in cancer cell studies. Additionally, RG-13022 has been described to inhibit EGF, platelet-dervied growth (PDGF) signaling, and PDGF enhanced DNA synthesis. RG-13022 is an inhibitor of EGFR and PDGFR.
For research and scientific purpose only, not for human use.
RG-13022 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 1 µM in HT-22 cells.
Product Name: RG-13022 |cas: 136831-48-6 |cat number: DC9857 |Molecule Formular: C16H14N2O2 |MW: 266.3 |purity>98%
RG-13022 is a Tyrosine kinase tyrphostin. Reports indicate that RG-13022 suppresses epidermal growth factor (EGF)-stimulated cancer cell proliferation in cancer cell studies. Additionally, RG-13022 has been described to inhibit EGF, platelet-dervied growth (PDGF) signaling, and PDGF enhanced DNA synthesis. RG-13022 is an inhibitor of EGFR and PDGFR.
For research and scientific purpose only, not for human use.
NS638|NS-638|Ca(2+)-channel blocker
NS638|NS-638|Ca(2+)-channel blocker
NS638 is a Ca(2+)-channel blocker.
Product Name: NS638 |cas: 150493-34-8 |cat number: DC9856 |Molecule Formular: C15H11ClF3N3 |MW: 325.72 |purity>98%
For research and scientific purpose only, not for human use.
NS638 is a Ca(2+)-channel blocker.
Product Name: NS638 |cas: 150493-34-8 |cat number: DC9856 |Molecule Formular: C15H11ClF3N3 |MW: 325.72 |purity>98%
For research and scientific purpose only, not for human use.
GK921|GK-921|TGase 2 inhibitor
GK921|GK-921|TGase 2 inhibitor
GK921 is a transglutaminase 2 (TGase 2) inhibitor with average GI50 of 0.9 uM in cancer cell lines.
Product Name: GK921 |cas: 1025015-40-0 |cat number: DC9855 |Molecule Formular: C21H20N4O |MW: 344.41 |purity>98%
GK921 is a transglutaminase 2 (TGase 2) inhibitor with average GI50 of 0.9 uM in cancer cell lines.
GK921 inhibited the tgase 2-induced polymerization of I-κBα and p53 in vitro in a dose-dependent manner. Oral administration of GK921 (8 mg/kg) began when tumors reached a volume of 100 mm3 and proceeded for 5 days/week. after 64 days of treatment, tumor volumes were significantly different in GK921-treated mice and vehicle-treated controls.
For research and scientific purpose only, not for human use.
GK921 is a transglutaminase 2 (TGase 2) inhibitor with average GI50 of 0.9 uM in cancer cell lines.
Product Name: GK921 |cas: 1025015-40-0 |cat number: DC9855 |Molecule Formular: C21H20N4O |MW: 344.41 |purity>98%
GK921 is a transglutaminase 2 (TGase 2) inhibitor with average GI50 of 0.9 uM in cancer cell lines.
GK921 inhibited the tgase 2-induced polymerization of I-κBα and p53 in vitro in a dose-dependent manner. Oral administration of GK921 (8 mg/kg) began when tumors reached a volume of 100 mm3 and proceeded for 5 days/week. after 64 days of treatment, tumor volumes were significantly different in GK921-treated mice and vehicle-treated controls.
For research and scientific purpose only, not for human use.
SAR407899|SAR-407899|ROCK inhibitor
SAR407899|SAR-407899|ROCK inhibitor
SAR407899 is a potent, ATP-competitive ROCK inhibitor woth Ki value of 36 nM/41 nM for human ROCK/Rat ROCK respectively.
Product Name: SAR407899 |cas: 923359-38-0 |cat number: DC9854 |Molecule Formular: C14H16N2O2 |MW: 244.29 |purity>98%
SAR407899 is a potent, ATP-competitive ROCK inhibitor woth Ki value of 36 nM/41 nM for human ROCK/Rat ROCK respectively.
in vitro: SAR407899 is highly selective in panel of 117 receptor and enzyme targets. SAR407899 is ≈8-fold more active than fasudil. In vitro, SAR407899 demonstrated concentration-dependent inhibition of Rho-kinase–mediated phosphorylation of myosin phosphatase, thrombin-induced stress fiber formation, platelet-derived growth factor–induced proliferation, and monocyte chemotactic protein-1–stimulated chemotaxis. SAR407899 potently (mean IC50 values: 122 to 280 nM) and species-independently relaxed precontracted isolated arteries of different species and different vascular beds [1]. SAR407899 dose-dependently relaxed the pre-contracted corpora cavernosa in all species, with similar potency and efficacy in healthy vs diabetic rats, WKY vs SHR rats, healthy vs diabetic rabbits (IC(50) range from 0.05 to 0.29 μM, Emax range 89 to 97%) [3].
in vivo: Over the dose range 3 to 30 mg/kg PO, SAR407899 lowered blood pressure in a variety of rodent models of arterial hypertension. SAR407899 was more effective than Y27632 in reducing ET-1-induced vasoconstriction in ZDF rat renal resistance arteries. Maximum ET-1-induced vasoconstriction in SAR407899-treated and Y27632-treated human renal resistance arteries was 23±5 and 48±6% of control values, respectively.
For research and scientific purpose only, not for human use.
SAR407899 is a potent, ATP-competitive ROCK inhibitor woth Ki value of 36 nM/41 nM for human ROCK/Rat ROCK respectively.
Product Name: SAR407899 |cas: 923359-38-0 |cat number: DC9854 |Molecule Formular: C14H16N2O2 |MW: 244.29 |purity>98%
SAR407899 is a potent, ATP-competitive ROCK inhibitor woth Ki value of 36 nM/41 nM for human ROCK/Rat ROCK respectively.
in vitro: SAR407899 is highly selective in panel of 117 receptor and enzyme targets. SAR407899 is ≈8-fold more active than fasudil. In vitro, SAR407899 demonstrated concentration-dependent inhibition of Rho-kinase–mediated phosphorylation of myosin phosphatase, thrombin-induced stress fiber formation, platelet-derived growth factor–induced proliferation, and monocyte chemotactic protein-1–stimulated chemotaxis. SAR407899 potently (mean IC50 values: 122 to 280 nM) and species-independently relaxed precontracted isolated arteries of different species and different vascular beds [1]. SAR407899 dose-dependently relaxed the pre-contracted corpora cavernosa in all species, with similar potency and efficacy in healthy vs diabetic rats, WKY vs SHR rats, healthy vs diabetic rabbits (IC(50) range from 0.05 to 0.29 μM, Emax range 89 to 97%) [3].
in vivo: Over the dose range 3 to 30 mg/kg PO, SAR407899 lowered blood pressure in a variety of rodent models of arterial hypertension. SAR407899 was more effective than Y27632 in reducing ET-1-induced vasoconstriction in ZDF rat renal resistance arteries. Maximum ET-1-induced vasoconstriction in SAR407899-treated and Y27632-treated human renal resistance arteries was 23±5 and 48±6% of control values, respectively.
For research and scientific purpose only, not for human use.
BM212|BM-212|MmpL3 inhibitor
BM212|BM-212|MmpL3 inhibitor
BM-212 is a potent antimycobacterial agent and MmpL3 inhibitor.
Product Name: BM212 |cas: 146204-42-4 |cat number: DC9853 |Molecule Formular: C23H25Cl2N3 |MW: 414.374 |purity>98%
BM-212 is a potent antimycobacterial agent and MmpL3 inhibitor. BM-212 was shown to possess strong inhibitory activity against both Mycobacterium tuberculosis and some nontuberculosis mycobacteria. BM212 was inhibitory to drug-resistant mycobacteria and also exerted bactericidal activity against intracellular bacilli residing in the U937 human histiocytic lymphoma cell line.
For research and scientific purpose only, not for human use.
BM-212 is a potent antimycobacterial agent and MmpL3 inhibitor.
Product Name: BM212 |cas: 146204-42-4 |cat number: DC9853 |Molecule Formular: C23H25Cl2N3 |MW: 414.374 |purity>98%
BM-212 is a potent antimycobacterial agent and MmpL3 inhibitor. BM-212 was shown to possess strong inhibitory activity against both Mycobacterium tuberculosis and some nontuberculosis mycobacteria. BM212 was inhibitory to drug-resistant mycobacteria and also exerted bactericidal activity against intracellular bacilli residing in the U937 human histiocytic lymphoma cell line.
For research and scientific purpose only, not for human use.
Ro 25-6981|NMDA receptors NR1C & NR2B blocker
Ro 25-6981|NMDA receptors NR1C & NR2B blocker
Ro 25-6981 is a potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit.
Product Name: Ro 25-6981 maleate |cas: 1312991-76-6 |cat number: DC9852 |Molecule Formular: C22H29NO2.C4H4O4 |MW: 455.55 |purity>98%
Ro 25-6981 is a potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit. IC50 values are 0.009 and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A respectively.
in vitro: Ro 25-6981 inhibited 3H-MK-801 binding to rat forebrain membranes in a biphasic manner with IC50 values of 0.003 microM and 149 microM for high- (about 60%) and low-affinity sites, respectively. NMDA receptor subtypes expressed in Xenopus oocytes were blocked with IC50 values of 0.009 microM and 52 microM for the subunit combinations NR1C & NR2B and NR1C & NR2A, respectively, which indicated a >5000-fold selectivity [1]. Increasing the concentration of spermidine did not change the efficacy of RO 25-6981 and minimally changed the IC(50) value. Epsilon1Q336R receptors were more inhibited by ifenprodil and RO 25-9681 than wildtype epsilon1 receptors in ligand binding assays but not in functional assays.
in vivo: Intrathecal injection of Ro 25-6981 significantly enhanced the paw withdrawal mechanical threshold and paw withdrawal thermal latency after the operation. Significant change has been observed after intrathecal injection of 800.0 μg of Ro 25-6981 and at 2h after operation in the oblique pull test degree and BBB rating score. Pretreatment of Ro 25-6981 decreased the high level expression of NR2B with tyrosine phosphorylation in spinal dorsal horn of the rat model after the operation.
For research and scientific purpose only, not for human use.
Ro 25-6981 is a potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit.
Product Name: Ro 25-6981 maleate |cas: 1312991-76-6 |cat number: DC9852 |Molecule Formular: C22H29NO2.C4H4O4 |MW: 455.55 |purity>98%
Ro 25-6981 is a potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit. IC50 values are 0.009 and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A respectively.
in vitro: Ro 25-6981 inhibited 3H-MK-801 binding to rat forebrain membranes in a biphasic manner with IC50 values of 0.003 microM and 149 microM for high- (about 60%) and low-affinity sites, respectively. NMDA receptor subtypes expressed in Xenopus oocytes were blocked with IC50 values of 0.009 microM and 52 microM for the subunit combinations NR1C & NR2B and NR1C & NR2A, respectively, which indicated a >5000-fold selectivity [1]. Increasing the concentration of spermidine did not change the efficacy of RO 25-6981 and minimally changed the IC(50) value. Epsilon1Q336R receptors were more inhibited by ifenprodil and RO 25-9681 than wildtype epsilon1 receptors in ligand binding assays but not in functional assays.
in vivo: Intrathecal injection of Ro 25-6981 significantly enhanced the paw withdrawal mechanical threshold and paw withdrawal thermal latency after the operation. Significant change has been observed after intrathecal injection of 800.0 μg of Ro 25-6981 and at 2h after operation in the oblique pull test degree and BBB rating score. Pretreatment of Ro 25-6981 decreased the high level expression of NR2B with tyrosine phosphorylation in spinal dorsal horn of the rat model after the operation.
For research and scientific purpose only, not for human use.
Ro 25-6981|NMDA receptors NR1C & NR2B blocker
Ro 25-6981|NMDA receptors NR1C & NR2B blocker
Ro 25-6981 is a potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit.
Product Name: Ro 25-6981 |cas: 169274-78-6 |cat number: DC9851 |Molecule Formular: C22H29NO2 |MW: 339.47 |purity>98%
Ro 25-6981 is a potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit. IC50 values are 0.009 and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A respectively.
in vitro: Ro 25-6981 inhibited 3H-MK-801 binding to rat forebrain membranes in a biphasic manner with IC50 values of 0.003 microM and 149 microM for high- (about 60%) and low-affinity sites, respectively. NMDA receptor subtypes expressed in Xenopus oocytes were blocked with IC50 values of 0.009 microM and 52 microM for the subunit combinations NR1C & NR2B and NR1C & NR2A, respectively, which indicated a >5000-fold selectivity [1]. Increasing the concentration of spermidine did not change the efficacy of RO 25-6981 and minimally changed the IC(50) value. Epsilon1Q336R receptors were more inhibited by ifenprodil and RO 25-9681 than wildtype epsilon1 receptors in ligand binding assays but not in functional assays.
in vivo: Intrathecal injection of Ro 25-6981 significantly enhanced the paw withdrawal mechanical threshold and paw withdrawal thermal latency after the operation. Significant change has been observed after intrathecal injection of 800.0 μg of Ro 25-6981 and at 2h after operation in the oblique pull test degree and BBB rating score. Pretreatment of Ro 25-6981 decreased the high level expression of NR2B with tyrosine phosphorylation in spinal dorsal horn of the rat model after the operation.
For research and scientific purpose only, not for human use.
Ro 25-6981 is a potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit.
Product Name: Ro 25-6981 |cas: 169274-78-6 |cat number: DC9851 |Molecule Formular: C22H29NO2 |MW: 339.47 |purity>98%
Ro 25-6981 is a potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit. IC50 values are 0.009 and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A respectively.
in vitro: Ro 25-6981 inhibited 3H-MK-801 binding to rat forebrain membranes in a biphasic manner with IC50 values of 0.003 microM and 149 microM for high- (about 60%) and low-affinity sites, respectively. NMDA receptor subtypes expressed in Xenopus oocytes were blocked with IC50 values of 0.009 microM and 52 microM for the subunit combinations NR1C & NR2B and NR1C & NR2A, respectively, which indicated a >5000-fold selectivity [1]. Increasing the concentration of spermidine did not change the efficacy of RO 25-6981 and minimally changed the IC(50) value. Epsilon1Q336R receptors were more inhibited by ifenprodil and RO 25-9681 than wildtype epsilon1 receptors in ligand binding assays but not in functional assays.
in vivo: Intrathecal injection of Ro 25-6981 significantly enhanced the paw withdrawal mechanical threshold and paw withdrawal thermal latency after the operation. Significant change has been observed after intrathecal injection of 800.0 μg of Ro 25-6981 and at 2h after operation in the oblique pull test degree and BBB rating score. Pretreatment of Ro 25-6981 decreased the high level expression of NR2B with tyrosine phosphorylation in spinal dorsal horn of the rat model after the operation.
For research and scientific purpose only, not for human use.
D-3263 HCl|D3263 HCl||Trp-p8 agonist
D-3263|D3263||Trp-p8 agonist
D-3263 in stock, price: 600 USD/100mg. D3263 is a novel, orally bioavailable small molecule Trp-p8 agonist.
Product Name: D-3263 HCl |cas: 1008763-54-9 |cat number: DC9850 |Molecule Formular: C21H31N3O3 |MW: 409.95 |purity>98%
D-3263 hydrochloride is an orally bioavailable (transient receptor potential melastatin member 8) TRPM8 agonist.
D-3263 hydrochloride binds to and activates TRPM8, which may result in an increase in calcium and sodium entry; the disruption of calcium and sodium homeostasis; and the induction of cell death in TRPM8-expressing tumor cells. D-3263 hydrochloride may decrease dihydrotestosterone (DHT) levels, which may contribute to its inhibitory effects on prostate cancer and BPH.
For research and scientific purpose only, not for human use.
D-3263 in stock, price: 600 USD/100mg. D3263 is a novel, orally bioavailable small molecule Trp-p8 agonist.
Product Name: D-3263 HCl |cas: 1008763-54-9 |cat number: DC9850 |Molecule Formular: C21H31N3O3 |MW: 409.95 |purity>98%
D-3263 hydrochloride is an orally bioavailable (transient receptor potential melastatin member 8) TRPM8 agonist.
D-3263 hydrochloride binds to and activates TRPM8, which may result in an increase in calcium and sodium entry; the disruption of calcium and sodium homeostasis; and the induction of cell death in TRPM8-expressing tumor cells. D-3263 hydrochloride may decrease dihydrotestosterone (DHT) levels, which may contribute to its inhibitory effects on prostate cancer and BPH.
For research and scientific purpose only, not for human use.
D-3263|D3263||Trp-p8 agonist
D-3263|D3263||Trp-p8 agonist
D-3263 in stock, price: 600 USD/100mg. D3263 is a novel, orally bioavailable small molecule Trp-p8 agonist..
Product Name: D-3263 |cas: 127910-31-0 |cat number: DC9849 |Molecule Formular: C21H31N3O3 |MW: 373.24 |purity>98%
D3263 as a small molecule compound for the treatment of solid tumors which are refractory to standard treatments.Treat advanced solid tumors; Treat solid tumors that are refractory to standard therapies
For research and scientific purpose only, not for human use.
D-3263 in stock, price: 600 USD/100mg. D3263 is a novel, orally bioavailable small molecule Trp-p8 agonist..
Product Name: D-3263 |cas: 127910-31-0 |cat number: DC9849 |Molecule Formular: C21H31N3O3 |MW: 373.24 |purity>98%
D3263 as a small molecule compound for the treatment of solid tumors which are refractory to standard treatments.Treat advanced solid tumors; Treat solid tumors that are refractory to standard therapies
For research and scientific purpose only, not for human use.
CGP37849|CGP-37849|NMDA receptor antagonist
CGP37849|CGP-37849|NMDA receptor antagonist
CGP37849 is a potent, selective and competitive NMDA receptor antagonist (Ki = 35 nM). Anticonvulsive following oral administration in vivo.
Product Name: CGP37849 |cas: 127910-31-0 |cat number: DC9849 |Molecule Formular: C6H12NO5P |MW: 209.14 |purity>98%
CGP-37849 is a competitive antagonist at the NMDA receptor. It is a potent, orally active anticonvulsant in animal models, and was researched for the treatment of epilepsy. It also has neuroprotective activity and shows antidepressant and anxiolytic effects.
For research and scientific purpose only, not for human use.
CGP37849 is a potent, selective and competitive NMDA receptor antagonist (Ki = 35 nM). Anticonvulsive following oral administration in vivo.
Product Name: CGP37849 |cas: 127910-31-0 |cat number: DC9849 |Molecule Formular: C6H12NO5P |MW: 209.14 |purity>98%
CGP-37849 is a competitive antagonist at the NMDA receptor. It is a potent, orally active anticonvulsant in animal models, and was researched for the treatment of epilepsy. It also has neuroprotective activity and shows antidepressant and anxiolytic effects.
For research and scientific purpose only, not for human use.
Ebselen|cas 60940-34-3|DC Chemicals
Ebselen|cas 60940-34-3|DC Chemicals
Ebselen is a selenium-based inhibitor of protein kinase C, NADPH, 5-lipoxygenase, cyclooxygenase (COX) and NADPH oxidase.
Product Name: Ebselen |cas: 60940-34-3 |cat number: DC9848 |Molecule Formular: C13H9NOSe |MW: 274.2 |purity>98%
Selenium-based inhibitor of protein kinase C, NADPH, 5-lipoxygenase, cyclooxygenase (COX) and NADPH oxidase. Anti-inflammatory antioxidant. Mimics glutathione peroxidase. Inhibits oxidative modifications of low density lipoproteins (LDL). Protects cerebellar granule neurons against 4-hydroxynonenal-induced neuronal death.
For research only, not for human use.
Ebselen is a selenium-based inhibitor of protein kinase C, NADPH, 5-lipoxygenase, cyclooxygenase (COX) and NADPH oxidase.
Product Name: Ebselen |cas: 60940-34-3 |cat number: DC9848 |Molecule Formular: C13H9NOSe |MW: 274.2 |purity>98%
Selenium-based inhibitor of protein kinase C, NADPH, 5-lipoxygenase, cyclooxygenase (COX) and NADPH oxidase. Anti-inflammatory antioxidant. Mimics glutathione peroxidase. Inhibits oxidative modifications of low density lipoproteins (LDL). Protects cerebellar granule neurons against 4-hydroxynonenal-induced neuronal death.
For research only, not for human use.
Vesnarinone|OPC8212|OPC-8212|PDE3 Inhibitor
Vesnarinone|OPC8212|OPC-8212|PDE3 Inhibitor
Vesnarinone is a quinolinone derivative, and its pharmacodynamic effects include inhibition of phosphodiesterase III (PDE3) activity, increases in calcium flux and decreases in potassium flux.
Product Name: Vesnarinone |cas: 81840-15-5 |cat number: DC9847 |Molecule Formular: C22H25N3O4 |MW: 395.45 |purity>98%
Vesnarinone is a quinolinone derivative, and its pharmacodynamic effects include inhibition of phosphodiesterase III (PDE3) activity, increases in calcium flux and decreases in potassium flux.
in vitro: HERG current is inhibited by Vesnarinone with an IC50 of 1.1 μM, whereas KvLQT1/minK current is not significantly depressed by Vesnarinone even at 30 μM. The IC50 value for Vesnarinone inhibition of HERG channels is 1 μM. The IC50 for Vesnarinone inhibition of PDE is reported to be 300 μM. Vesnarinone is a novel cytokine inhibitor, for the treatment of lung fibrosis using a murine model of bleomycin (BLM)-induced pulmonary fibrosis. Vesnarinone inhibits BLM-induced pulmonary fibrosis, at least in part, by the inhibition of acute lung injuries in the early phase. [2] Vesnarinone is a new and novel inotropic drug that has unique and complex mechanisms of action. Vesnarinone inhibits phosphodiesterase, thereby leading to increased intracellular calcium, and also affects numerous myocardial ion channels, resulting in the prolongation of the opening time of sodium channels and the decrease in the delayed outward and inward rectifying potassium current. Vesnarinone has also demonstrated significant effects on cytokine production, which may account for some of its observed clinical benefits.[3] Vesnarinone plays an important role in the regulation of cytokines and suggest that the reduction of cytokine release may contribute to the beneficial effects of the drug in the treatment of heart failure. Vesnarinone inhibits the production of TFN-a and IFN-y by LPS stimulated whole blood from patients with heart failure and from healthy volunteers.
in vivo: Vesnarinone reduces the circulating levels of TNF-α. Cumulative evidence showed that a variety of cytokine are involved in the pathogenesis of pulmonary fibrosis.
For research only, not for human use.
Vesnarinone is a quinolinone derivative, and its pharmacodynamic effects include inhibition of phosphodiesterase III (PDE3) activity, increases in calcium flux and decreases in potassium flux.
Product Name: Vesnarinone |cas: 81840-15-5 |cat number: DC9847 |Molecule Formular: C22H25N3O4 |MW: 395.45 |purity>98%
Vesnarinone is a quinolinone derivative, and its pharmacodynamic effects include inhibition of phosphodiesterase III (PDE3) activity, increases in calcium flux and decreases in potassium flux.
in vitro: HERG current is inhibited by Vesnarinone with an IC50 of 1.1 μM, whereas KvLQT1/minK current is not significantly depressed by Vesnarinone even at 30 μM. The IC50 value for Vesnarinone inhibition of HERG channels is 1 μM. The IC50 for Vesnarinone inhibition of PDE is reported to be 300 μM. Vesnarinone is a novel cytokine inhibitor, for the treatment of lung fibrosis using a murine model of bleomycin (BLM)-induced pulmonary fibrosis. Vesnarinone inhibits BLM-induced pulmonary fibrosis, at least in part, by the inhibition of acute lung injuries in the early phase. [2] Vesnarinone is a new and novel inotropic drug that has unique and complex mechanisms of action. Vesnarinone inhibits phosphodiesterase, thereby leading to increased intracellular calcium, and also affects numerous myocardial ion channels, resulting in the prolongation of the opening time of sodium channels and the decrease in the delayed outward and inward rectifying potassium current. Vesnarinone has also demonstrated significant effects on cytokine production, which may account for some of its observed clinical benefits.[3] Vesnarinone plays an important role in the regulation of cytokines and suggest that the reduction of cytokine release may contribute to the beneficial effects of the drug in the treatment of heart failure. Vesnarinone inhibits the production of TFN-a and IFN-y by LPS stimulated whole blood from patients with heart failure and from healthy volunteers.
in vivo: Vesnarinone reduces the circulating levels of TNF-α. Cumulative evidence showed that a variety of cytokine are involved in the pathogenesis of pulmonary fibrosis.
For research only, not for human use.
BS-181|BS181|CDK7 Inhibitor|DC Chemicals
BS-181|BS181|CDK7 Inhibitor|DC Chemicals
BS-181 in stock,price: 450 USD/100mg. BS-181 is a highly selective CDK7 inhibitor with IC50 of 21 nM. ; >40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.
Product Name: BS-181 free base |cas: 1092443-52-1 |cat number: DC9846 |Molecule Formular: C22H32N6 |MW: 380.53 |purity>98%
BS-181 is a highly selective CDK7 inhibitor with IC50 of 21 nM. ; >40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.
IC50 Value: 21 nM
in vitro: BS-181 is a small molecule inhibitor of CDK7 in a cell-free environment, which displays more potential activity than roscovitine with IC 50 of 510 nM. Among the CDKs and other 69 kinases from many different classes, BS-181 shows high inhibitory selectivity for CDK7, inhibits CDK2 at concentrations lower than 1 μM which being inhibited 35-fold less potently (IC50 with 880 nM) than CDK7, shows slight inhibition for CDK1, CDK4, CDK5, CDK6 and CDK9 with IC50 values higher than 3.0 μM, and only shows inhibition for several kinases from other classes at high concentrations (>10 μM). BS-181 promotes cell cycle arrest and inhibits the cancer cell growth of a range of tumor types, including breast, lung, prostate and colorectal cancer with IC50 in the range of 11.5-37 μM. In MCF-7 cells, BS-181 inhibits the phosphorylation of the CDK7 substrate RNA polymerase II COOH-terminal domain (CTD), and promotes cell cycle arrest and apoptosis to inhibit the growth of cancer cell lines.
in vivo: BS-181 is stable in vivo with a plasma elimination half-life in mice of 405 minutes after i.p. administration of 10 mg/kg. BS-181 inhibits the growth of MCF-7 xenografts in the nude mice model in a dose-dependent manner, with 25% and 50% reduction in tumor growth after 2 weeks of treatment at 10 mg/kg/day and 20 mg/kg/day, respectively without apparent toxicity. For the detailed information of BS-181 hydrochloride, the solubility of BS-181 hydrochloride in water, the solubility of BS-181 hydrochloride in DMSO, the solubility of BS-181 hydrochloride in PBS buffer, the animal experiment (test) of BS-181 hydrochloride, the cell expriment (test) of BS-181 hydrochloride, the in vivo, in vitro and clinical trial test of BS-181 hydrochloride, the EC50, IC50,and affinity,of BS-181 hydrochloride, For the detailed information of BS-181 hydrochloride, the solubility of BS-181 hydrochloride in water, the solubility of BS-181 hydrochloride in DMSO, the solubility of BS-181 hydrochloride in PBS buffer, the animal experiment (test) of BS-181 hydrochloride, the cell expriment (test) of BS-181 hydrochloride, the in vivo, in vitro and clinical trial test of BS-181 hydrochloride, the EC50, IC50,and affinity,of BS-181 hydrochloride, Please contact DC Chemicals.
For research only, not for human use.
BS-181 in stock,price: 450 USD/100mg. BS-181 is a highly selective CDK7 inhibitor with IC50 of 21 nM. ; >40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.
Product Name: BS-181 free base |cas: 1092443-52-1 |cat number: DC9846 |Molecule Formular: C22H32N6 |MW: 380.53 |purity>98%
BS-181 is a highly selective CDK7 inhibitor with IC50 of 21 nM. ; >40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.
IC50 Value: 21 nM
in vitro: BS-181 is a small molecule inhibitor of CDK7 in a cell-free environment, which displays more potential activity than roscovitine with IC 50 of 510 nM. Among the CDKs and other 69 kinases from many different classes, BS-181 shows high inhibitory selectivity for CDK7, inhibits CDK2 at concentrations lower than 1 μM which being inhibited 35-fold less potently (IC50 with 880 nM) than CDK7, shows slight inhibition for CDK1, CDK4, CDK5, CDK6 and CDK9 with IC50 values higher than 3.0 μM, and only shows inhibition for several kinases from other classes at high concentrations (>10 μM). BS-181 promotes cell cycle arrest and inhibits the cancer cell growth of a range of tumor types, including breast, lung, prostate and colorectal cancer with IC50 in the range of 11.5-37 μM. In MCF-7 cells, BS-181 inhibits the phosphorylation of the CDK7 substrate RNA polymerase II COOH-terminal domain (CTD), and promotes cell cycle arrest and apoptosis to inhibit the growth of cancer cell lines.
in vivo: BS-181 is stable in vivo with a plasma elimination half-life in mice of 405 minutes after i.p. administration of 10 mg/kg. BS-181 inhibits the growth of MCF-7 xenografts in the nude mice model in a dose-dependent manner, with 25% and 50% reduction in tumor growth after 2 weeks of treatment at 10 mg/kg/day and 20 mg/kg/day, respectively without apparent toxicity. For the detailed information of BS-181 hydrochloride, the solubility of BS-181 hydrochloride in water, the solubility of BS-181 hydrochloride in DMSO, the solubility of BS-181 hydrochloride in PBS buffer, the animal experiment (test) of BS-181 hydrochloride, the cell expriment (test) of BS-181 hydrochloride, the in vivo, in vitro and clinical trial test of BS-181 hydrochloride, the EC50, IC50,and affinity,of BS-181 hydrochloride, For the detailed information of BS-181 hydrochloride, the solubility of BS-181 hydrochloride in water, the solubility of BS-181 hydrochloride in DMSO, the solubility of BS-181 hydrochloride in PBS buffer, the animal experiment (test) of BS-181 hydrochloride, the cell expriment (test) of BS-181 hydrochloride, the in vivo, in vitro and clinical trial test of BS-181 hydrochloride, the EC50, IC50,and affinity,of BS-181 hydrochloride, Please contact DC Chemicals.
For research only, not for human use.
FITM|mGlu1 inhibitor|cas 932737-65-0
FITM|mGlu1 inhibitor|cas 932737-65-0
FITM in stock. FITM is a nove mGlu1 inhibitor. FITM shows high affinity (Ki = 2.5 nM, fig. S2) and selectivity for mGlu1 over mGlu5.
Product Name: FITM |cas: 932737-65-0 |cat number: DC9845 |Molecule Formular: C18H18FN5OS |MW: 371.43 |purity>98%
FITM is a nove mGlu1 inhibitor. FITM shows high affinity (Ki = 2.5 nM, fig. S2) and selectivity for mGlu1 over mGlu5.
For research only, not for human use.
FITM in stock. FITM is a nove mGlu1 inhibitor. FITM shows high affinity (Ki = 2.5 nM, fig. S2) and selectivity for mGlu1 over mGlu5.
Product Name: FITM |cas: 932737-65-0 |cat number: DC9845 |Molecule Formular: C18H18FN5OS |MW: 371.43 |purity>98%
FITM is a nove mGlu1 inhibitor. FITM shows high affinity (Ki = 2.5 nM, fig. S2) and selectivity for mGlu1 over mGlu5.
For research only, not for human use.
STK321130（FLT3-IN-2）|FLT3 inhibitor|CAS 923562-23-6
STK321130（FLT3-IN-2）|FLT3 inhibitor|CAS 923562-23-6
STK321130（FLT3-IN-2）in stock, price: 500 USD/100mg. STK321130（FLT3-IN-2）is potent FLT3 inhibitor
Product Name: STK321130（FLT3-IN-2) |cas: 923562-23-6 |cat number: DC9844 |Molecule Formular: C21H16ClF3N4 |MW: 416.1 |purity>98%
STK321130（FLT3-IN-2）is potent FLT3 inhibitor
For research only, not for human use.
STK321130（FLT3-IN-2）in stock, price: 500 USD/100mg. STK321130（FLT3-IN-2）is potent FLT3 inhibitor
Product Name: STK321130（FLT3-IN-2) |cas: 923562-23-6 |cat number: DC9844 |Molecule Formular: C21H16ClF3N4 |MW: 416.1 |purity>98%
STK321130（FLT3-IN-2）is potent FLT3 inhibitor
For research only, not for human use.
AKR1C3 Inhibitor 5f|cas 1275482-57-9
AKR1C3 Inhibitor 5f|cas 1275482-57-9
A highly potent and selective inhibitor of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3.
Product Name: AKR1C3 Inhibitor 5f |cas: 1275482-57-9 |cat number: DC9843 |Molecule Formular: C14H13NO3 |MW: 243.26 |purity>98%
A cell-permeable 3-phenyl-aminobenzoate compound that acts as a potent, competitive, reversible, active-site targeting inhibitor of aldo-keto reductase 1C3 (AKR1C3; type 5 17β-hydroxysteroid dehydrogenase) (IC50 = 2.65µM) with excellent selectivity over other closely related human AKR isoforms (IC50 = 2.65µM, 84.4µM, for AKR1C3, AKR1C2, respectively. Exhibits a weak inhibitory effect on cyclooxygenase 1 and 2 (IC50 = 100 µM). Shown to efficiently block the AKR1C3-mediated production of testosterone in LNCaP-AKR1C3 cells.
For research only, not for human use.
A highly potent and selective inhibitor of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3.
Product Name: AKR1C3 Inhibitor 5f |cas: 1275482-57-9 |cat number: DC9843 |Molecule Formular: C14H13NO3 |MW: 243.26 |purity>98%
A cell-permeable 3-phenyl-aminobenzoate compound that acts as a potent, competitive, reversible, active-site targeting inhibitor of aldo-keto reductase 1C3 (AKR1C3; type 5 17β-hydroxysteroid dehydrogenase) (IC50 = 2.65µM) with excellent selectivity over other closely related human AKR isoforms (IC50 = 2.65µM, 84.4µM, for AKR1C3, AKR1C2, respectively. Exhibits a weak inhibitory effect on cyclooxygenase 1 and 2 (IC50 = 100 µM). Shown to efficiently block the AKR1C3-mediated production of testosterone in LNCaP-AKR1C3 cells.
For research only, not for human use.
T0901317|T-0901317|LXR agonist
T0901317|T-0901317|LXR agonist.
T0901317 in stock, price: 300USD/100mg. T0901317 is a potent, high affinity liver X receptor (LXR) agonist (EC50 ~ 50 nM, Kd values are 7 and 22 nM for LXR-α and LXR-β respectively).
Product Name: T0901317 |cas: 293754-55-9 |cat number: DC9842 |Molecule Formular: C17H12F9NO3S |MW: 481.33 |purity>98%
Potent, high affinity liver X receptor (LXR) agonist (EC50 ~ 50 nM, Kd values are 7 and 22 nM for LXR-α and LXR-β respectively). Upregulates expression of the ABCA1 gene associated with cholesterol efflux regulation and HDL metabolism. Decreases amyloid-β production in primary neurons in vitro. Displays an EC50 of ~ 5 μM for activation of bile acid farnesoid X receptors (FXRs); 10-fold more potent than natural FXR ligand chenodeoxycholic acid. Also exhibits inverse agonist activity at constitutive androstane receptors (CAR).
For research only, not for human use.
T0901317 in stock, price: 300USD/100mg. T0901317 is a potent, high affinity liver X receptor (LXR) agonist (EC50 ~ 50 nM, Kd values are 7 and 22 nM for LXR-α and LXR-β respectively).
Product Name: T0901317 |cas: 293754-55-9 |cat number: DC9842 |Molecule Formular: C17H12F9NO3S |MW: 481.33 |purity>98%
Potent, high affinity liver X receptor (LXR) agonist (EC50 ~ 50 nM, Kd values are 7 and 22 nM for LXR-α and LXR-β respectively). Upregulates expression of the ABCA1 gene associated with cholesterol efflux regulation and HDL metabolism. Decreases amyloid-β production in primary neurons in vitro. Displays an EC50 of ~ 5 μM for activation of bile acid farnesoid X receptors (FXRs); 10-fold more potent than natural FXR ligand chenodeoxycholic acid. Also exhibits inverse agonist activity at constitutive androstane receptors (CAR).
For research only, not for human use.
Fostamatinib|R788|Syk inhibitor
Fostamatinib|R788|Syk inhibitor
R788 (Fostamatinib), a prodrug of the active metabolite R406, is a potent Syk inhibitor with IC50 of 41 nM.
Product Name: Fostamatinib(R788) |cas: 901119-35-5 |cat number: DC9841 |Molecule Formular: C23H26FN6O9P |MW: 580.46 |purity>98%
R788 is a methylene phosphate prodrug of R406, which can be rapidly converted to R406 in vivo. R406 (in vitro active form of R788) selectively inhibits Syk-dependent signaling with EC50 values ranging from 33 nM to 171 nM, more potently than Syk-independent pathways in different cells. R406 inhibits cellular proliferation of a variety of diffuse large B-cell lymphoma (DLBCL) cell lines with EC50 values ranging from 0.8 μM to 8.1 μM [2]. R406 treatment reduces basal phosphorylation of BLNK, Akt, glycogen synthase kinase-3 (GSK-3), forkhead box O (FOXO) and ERK not only in cells with high (TCL-002) but also in cells with low levels of phosphorylated Syk (TCL1-551). In addition, R406 completely inhibits the anti-IgM induced Bcr signal in TCL1 leukemias. Despite the higher levels of constitutively active Syk in TCL1 leukemias, R406 is not selectively cytotoxic to the leukemic cells .
in vivo: R788 effectively inhibits BCR signaling in vivo, resulting in reduced proliferation and survival of the malignant B cells and significantly prolonged survival of the treated animals.
For research only, not for human use.
R788 (Fostamatinib), a prodrug of the active metabolite R406, is a potent Syk inhibitor with IC50 of 41 nM.
Product Name: Fostamatinib(R788) |cas: 901119-35-5 |cat number: DC9841 |Molecule Formular: C23H26FN6O9P |MW: 580.46 |purity>98%
R788 is a methylene phosphate prodrug of R406, which can be rapidly converted to R406 in vivo. R406 (in vitro active form of R788) selectively inhibits Syk-dependent signaling with EC50 values ranging from 33 nM to 171 nM, more potently than Syk-independent pathways in different cells. R406 inhibits cellular proliferation of a variety of diffuse large B-cell lymphoma (DLBCL) cell lines with EC50 values ranging from 0.8 μM to 8.1 μM [2]. R406 treatment reduces basal phosphorylation of BLNK, Akt, glycogen synthase kinase-3 (GSK-3), forkhead box O (FOXO) and ERK not only in cells with high (TCL-002) but also in cells with low levels of phosphorylated Syk (TCL1-551). In addition, R406 completely inhibits the anti-IgM induced Bcr signal in TCL1 leukemias. Despite the higher levels of constitutively active Syk in TCL1 leukemias, R406 is not selectively cytotoxic to the leukemic cells .
in vivo: R788 effectively inhibits BCR signaling in vivo, resulting in reduced proliferation and survival of the malignant B cells and significantly prolonged survival of the treated animals.
For research only, not for human use.
AS 8351|AS8351|Induce reprogramming|for stem cell
AS 8351|AS8351|Induce reprogramming|for stem cell
AS8351 in stock, price: 300USD/100mg. AS 8351 induces reprogramming of human fetal lung fibroblasts into functional cardiomyocytes, in combination with CHIR 99021, A83-01, BIX 01294, SC1, Y-27632, OAC2, SU 16f and JNJ 10198409.
Product Name: AS-8351 |cas: 796-42-9 |cat number: DC9840 |Molecule Formular: C17H13N3O2 |MW: 291.3 |purity>98%
AS 8351 induces reprogramming of human fetal lung fibroblasts into functional cardiomyocytes, in combination with CHIR 99021, A83-01, BIX 01294, SC1, Y-27632, OAC2, SU 16f and JNJ 10198409. Iron chelator and putative inhibitor of KDM5B.
For research only, not for human use.
AS8351 in stock, price: 300USD/100mg. AS 8351 induces reprogramming of human fetal lung fibroblasts into functional cardiomyocytes, in combination with CHIR 99021, A83-01, BIX 01294, SC1, Y-27632, OAC2, SU 16f and JNJ 10198409.
Product Name: AS-8351 |cas: 796-42-9 |cat number: DC9840 |Molecule Formular: C17H13N3O2 |MW: 291.3 |purity>98%
AS 8351 induces reprogramming of human fetal lung fibroblasts into functional cardiomyocytes, in combination with CHIR 99021, A83-01, BIX 01294, SC1, Y-27632, OAC2, SU 16f and JNJ 10198409. Iron chelator and putative inhibitor of KDM5B.
For research only, not for human use.
Brassinin|Inducer of phase II enzymes
Brassinin|Inducer of phase II enzymes
Brassinin is a Inducer of phase II enzymes. Moderate and competitive indoleamine 2,3-dioxygenase inhibitor (Ki = 98 μM). Shows chemopreventive effects in vivo. Orally active.
Product Name: Brassinin |cas: 105748-59-2 |cat number: DC9839 |Molecule Formular: C11H12N2S2 |MW: 236.36 |purity>98%
Brassinin is a phytoalexin found in Chinese cabbage. An effective inhibitor of stage two skin carcinogenesis. Brassinin is an inducer of Phase II enzymes and inhibitor of chemically induced carcinogenesis.
For research only, not for human use.
Brassinin is a Inducer of phase II enzymes. Moderate and competitive indoleamine 2,3-dioxygenase inhibitor (Ki = 98 μM). Shows chemopreventive effects in vivo. Orally active.
Product Name: Brassinin |cas: 105748-59-2 |cat number: DC9839 |Molecule Formular: C11H12N2S2 |MW: 236.36 |purity>98%
Brassinin is a phytoalexin found in Chinese cabbage. An effective inhibitor of stage two skin carcinogenesis. Brassinin is an inducer of Phase II enzymes and inhibitor of chemically induced carcinogenesis.
For research only, not for human use.
Alsterpaullone|9-Nitropaullone|CDK inhibitor
Alsterpaullone|9-Nitropaullone|CDK inhibitor
Alsterpaullone in stock, price:650 USD/100mg. Alsterpaullone is a potent ATP-competitive and cell cycle cyclin-dependent kinase inhibitor, that is reported to be the most active Paullone.
Product Name: Alsterpaullone |cas: 237430-03-4 |cat number: DC9838 |Molecule Formular: C16H11N3O3 |MW: 293.28 |purity>98%
Alsterpaullone is a potent ATP-competitive and cell cycle cyclin-dependent kinase inhibitor, that is reported to be the most active Paullone. The paullones belong to a family of benzazepinones, and are described to highly inhibit neuronal CDK5/p25 and glycogen synthase kinase-3β (GSK-3β). Studies report that Alsterpaullone activates caspase-9 and enhances apoptosis in Jurkat cells, inhibits CDK5/p25-dependent phosphorylation of DARPP-32 in in vitro mouse striatum slices, and blocks the phosphorylation of Tau by GSK-3β.
For research only, not for human use.
Alsterpaullone in stock, price:650 USD/100mg. Alsterpaullone is a potent ATP-competitive and cell cycle cyclin-dependent kinase inhibitor, that is reported to be the most active Paullone.
Product Name: Alsterpaullone |cas: 237430-03-4 |cat number: DC9838 |Molecule Formular: C16H11N3O3 |MW: 293.28 |purity>98%
Alsterpaullone is a potent ATP-competitive and cell cycle cyclin-dependent kinase inhibitor, that is reported to be the most active Paullone. The paullones belong to a family of benzazepinones, and are described to highly inhibit neuronal CDK5/p25 and glycogen synthase kinase-3β (GSK-3β). Studies report that Alsterpaullone activates caspase-9 and enhances apoptosis in Jurkat cells, inhibits CDK5/p25-dependent phosphorylation of DARPP-32 in in vitro mouse striatum slices, and blocks the phosphorylation of Tau by GSK-3β.
For research only, not for human use.
LOXO-101|LOXO101|TRK inhibitor
LOXO-101|LOXO101|TRK inhibitor
LOXO-101 in stock,850 USD/100mg. LOXO-101 is a small molecule that was designed to block the ATP binding site of the TRK family of receptors, with 2 to 20 nM cellular potency against the TRKA, TRKB, and TRKC kinases.
Product Name: LOXO-101 sulfate |cas: 1223405-08-0 |cat number: DC9837 |Molecule Formular: C21H24F2N6O6S |MW: 526.51 |purity>98%
LOXO-101 is a small molecule that was designed to block the ATP binding site of the TRK family of receptors, with 2 to 20 nM cellular potency against the TRKA, TRKB, and TRKC kinases.
in vitro: LOXO-101 is an orally administered inhibitor of the TRK kinase and is highly selective only for the TRK family of receptors. LOXO-101 is evaluated for off-target kinase enzyme inhibition against a panel of 226 non-TRK kinases at a compound concentration of 1,000 nM and ATP concentrations near the Km for each enzyme. In the panel, LOXO-101 demonstrates greater than 50% inhibition for only one non-TRK kinase (TNK2 IC50, 576 nM). Measurement of proliferation following treatment with LOXO-101 demonstrates a dose-dependent inhibition of cell proliferation in all three cell lines. The IC50 is less than 100 nM for CUTO-3.29 and less than 10 nM for KM12 and MO-91, consistent with the known potency of this drug for the TRK kinase family. [1] LOXO-101 demonstrates potent and highly-selective inhibition of TRKA, TRKB, and TRKC over other kinase- and non-kinase targets. LOXO-101 is a potent, ATP-competitive TRK inhibitor with IC50s in low nanomolar range for inhibition of all TRK family members in binding and cellular assays, with 100x selectivity over other kinases. [2]
in vivo: Athymic nude mice injected with KM12 cells are treated with LOXO-101 orally daily for 2 weeks. Dose-dependent tumor inhibition is observed, demonstrating the ability of this selective compound to inhibit tumor growth in vivo.
For research only, not for human use.
LOXO-101 in stock,850 USD/100mg. LOXO-101 is a small molecule that was designed to block the ATP binding site of the TRK family of receptors, with 2 to 20 nM cellular potency against the TRKA, TRKB, and TRKC kinases.
Product Name: LOXO-101 sulfate |cas: 1223405-08-0 |cat number: DC9837 |Molecule Formular: C21H24F2N6O6S |MW: 526.51 |purity>98%
LOXO-101 is a small molecule that was designed to block the ATP binding site of the TRK family of receptors, with 2 to 20 nM cellular potency against the TRKA, TRKB, and TRKC kinases.
in vitro: LOXO-101 is an orally administered inhibitor of the TRK kinase and is highly selective only for the TRK family of receptors. LOXO-101 is evaluated for off-target kinase enzyme inhibition against a panel of 226 non-TRK kinases at a compound concentration of 1,000 nM and ATP concentrations near the Km for each enzyme. In the panel, LOXO-101 demonstrates greater than 50% inhibition for only one non-TRK kinase (TNK2 IC50, 576 nM). Measurement of proliferation following treatment with LOXO-101 demonstrates a dose-dependent inhibition of cell proliferation in all three cell lines. The IC50 is less than 100 nM for CUTO-3.29 and less than 10 nM for KM12 and MO-91, consistent with the known potency of this drug for the TRK kinase family. [1] LOXO-101 demonstrates potent and highly-selective inhibition of TRKA, TRKB, and TRKC over other kinase- and non-kinase targets. LOXO-101 is a potent, ATP-competitive TRK inhibitor with IC50s in low nanomolar range for inhibition of all TRK family members in binding and cellular assays, with 100x selectivity over other kinases. [2]
in vivo: Athymic nude mice injected with KM12 cells are treated with LOXO-101 orally daily for 2 weeks. Dose-dependent tumor inhibition is observed, demonstrating the ability of this selective compound to inhibit tumor growth in vivo.
For research only, not for human use.
Mivebresib|ABBV-075（ABBV075）|BET/MYC inhibitor
Mivebresib|ABBV-075（ABBV075）|BET/MYC inhibitor
Mivebresib in stock, 800 USD/100mg. Mivebresib is a novel BET family inhibitor, disrupts critical transcription programs that drive prostate cancer growth to induce potent anti-tumor activity in vitro and in vivo. Also a potent inhibitor of MYC and the TMPRSS2-ETS fusion proteins
Product Name: Mivebresib(ABBV-075） |cas: 1445993-26-9 |cat number: DC9836 |Molecule Formular: C22H19F2N3O4S |MW: 459.47 |purity>98%
Mivebresib is a novel BET family inhibitor, disrupts critical transcription programs that drive prostate cancer growth to induce potent anti-tumor activity in vitro and in vivo. Also a potent inhibitor of MYC and the TMPRSS2-ETS fusion proteins. Mivebresib inhibit DHT-stimulated transcription of AR target genes without significant effect on AR protein expression. In addition to blocking the transcription activation downstream of AR, Mivebresib is also a potent inhibitor of MYC and the TMPRSS2-ETS fusion proteins.
For research only, not for human use.
Mivebresib in stock, 800 USD/100mg. Mivebresib is a novel BET family inhibitor, disrupts critical transcription programs that drive prostate cancer growth to induce potent anti-tumor activity in vitro and in vivo. Also a potent inhibitor of MYC and the TMPRSS2-ETS fusion proteins
Product Name: Mivebresib(ABBV-075） |cas: 1445993-26-9 |cat number: DC9836 |Molecule Formular: C22H19F2N3O4S |MW: 459.47 |purity>98%
Mivebresib is a novel BET family inhibitor, disrupts critical transcription programs that drive prostate cancer growth to induce potent anti-tumor activity in vitro and in vivo. Also a potent inhibitor of MYC and the TMPRSS2-ETS fusion proteins. Mivebresib inhibit DHT-stimulated transcription of AR target genes without significant effect on AR protein expression. In addition to blocking the transcription activation downstream of AR, Mivebresib is also a potent inhibitor of MYC and the TMPRSS2-ETS fusion proteins.
For research only, not for human use.
Cytochalasin H|for actin polymerization studies
Cytochalasin H|for actin polymerization studies
Cytochalasin H in stock, 1300 USD/100mg. Cytochalasin H is a potent inhibitor of actin incorporation into filaments.
Product Name: Cytochalasin H |cas: 53760-19-3 |cat number: DC9835 |Molecule Formular: C30H39NO5 |MW: 493.6 |purity>98%
Cytochalasin H is a potent inhibitor of actin incorporation into filaments,a cell-permeable fungal toxin used in actin polymerization studies and cytological research. Cytochalasin H suppresses the production of reactive oxygen species by stimulated human neutrophils, blocks endocytosis of CD59 in lymphocytes, and shows anti-angiogenic activity both in vitro and in vivo.
For research only, not for human use.
Cytochalasin H in stock, 1300 USD/100mg. Cytochalasin H is a potent inhibitor of actin incorporation into filaments.
Product Name: Cytochalasin H |cas: 53760-19-3 |cat number: DC9835 |Molecule Formular: C30H39NO5 |MW: 493.6 |purity>98%
Cytochalasin H is a potent inhibitor of actin incorporation into filaments,a cell-permeable fungal toxin used in actin polymerization studies and cytological research. Cytochalasin H suppresses the production of reactive oxygen species by stimulated human neutrophils, blocks endocytosis of CD59 in lymphocytes, and shows anti-angiogenic activity both in vitro and in vivo.
For research only, not for human use.
Dioscin(CCRIS 4123; Collettiside III)
Dioscin(CCRIS 4123; Collettiside III)
Dioscin(CCRIS 4123; Collettiside III) is a natural steroid saponin derived from several plants, showing potent anti-cancer effect against a variety of tumor cell lines..
Product Name: Dioscin |cas: 19057-60-4 |cat number: DC9834 |Molecule Formular: C45H72O16 |MW: 869.04 |purity>98%
Dioscin(CCRIS 4123; Collettiside III) is a natural steroid saponin derived from several plants, showing potent anti-cancer effect against a variety of tumor cell lines
in vitro: dioscin (1, 2 and 4 μmol/L) could significantly inhibit the viability of LNCaP cells in a time- and concentration-dependent manner. Flow cytometry revealed that the apoptosis rate was increased after treatment of LNCaP cells with dioscin for 24 h, indicating that apoptosis was an important mechanism by which dioscin inhibited cancer. dioscin abrogated AKT phosphorylation, which subsequently impaired RANKL-induced nuclear factor-kappaB (NF-κB) signaling pathway and inhibited NFATc1 transcriptional activity. Moreover, in vivo studies further verified the bone protection activity of dioscin in osteolytic animal model. Dioscin reduced cell death and lactate dehydrogenase (LDH) release in cells subjected to I/R. I/R induced apoptosis and cytochrome c release from mitochondria to the cytosol and this was prevented by dioscin. In support, dioscin decreased Bax but increased Bcl-2 mRNA expression. Dioscin prevented I/R induced dissipation of ΔΨm.
For research only, not for human use.
Dioscin(CCRIS 4123; Collettiside III) is a natural steroid saponin derived from several plants, showing potent anti-cancer effect against a variety of tumor cell lines..
Product Name: Dioscin |cas: 19057-60-4 |cat number: DC9834 |Molecule Formular: C45H72O16 |MW: 869.04 |purity>98%
Dioscin(CCRIS 4123; Collettiside III) is a natural steroid saponin derived from several plants, showing potent anti-cancer effect against a variety of tumor cell lines
in vitro: dioscin (1, 2 and 4 μmol/L) could significantly inhibit the viability of LNCaP cells in a time- and concentration-dependent manner. Flow cytometry revealed that the apoptosis rate was increased after treatment of LNCaP cells with dioscin for 24 h, indicating that apoptosis was an important mechanism by which dioscin inhibited cancer. dioscin abrogated AKT phosphorylation, which subsequently impaired RANKL-induced nuclear factor-kappaB (NF-κB) signaling pathway and inhibited NFATc1 transcriptional activity. Moreover, in vivo studies further verified the bone protection activity of dioscin in osteolytic animal model. Dioscin reduced cell death and lactate dehydrogenase (LDH) release in cells subjected to I/R. I/R induced apoptosis and cytochrome c release from mitochondria to the cytosol and this was prevented by dioscin. In support, dioscin decreased Bax but increased Bcl-2 mRNA expression. Dioscin prevented I/R induced dissipation of ΔΨm.
For research only, not for human use.
(20S)-Protopanaxadiol|apoptosis inducer
(20S)-Protopanaxadiol|apoptosis inducer
(20S)-Protopanaxadiol (20-Epiprotopanaxadiol) is an aglycon metabolic derivative of the protopanaxadiol-type ginseng saponin; apoptosis inducer.
Product Name: (20S)-Protopanaxadiol |cas: 30636-90-9 |cat number: DC9833 |Molecule Formular: C30H52O3 |MW: 460.73 |purity>98%
(20S)-Protopanaxadiol (20-Epiprotopanaxadiol) is an aglycon metabolic derivative of the protopanaxadiol-type ginseng saponin; apoptosis inducer.
Target: apoptosis inducer
(20S)-Protopanaxadiol was used to induce cytotoxicity for two human glioma cell lines, SF188 and U87MG. For the SF188 cells, (20S)-Protopanaxadiol activated caspases-3, -8, -7, and -9 within 3 h and induced rapid apoptosis, which could be partially inhibited by a general caspase blocker and completely abolished when the caspase blocker was used in combination with an antioxidant. (20S)-Protopanaxadiol also induced cell death in U87MG cells but did not activate any caspases in these cells [. aPPD was able to inhibit P-gp activity as potently as verapamil on MDR cells. The blockage of P-gp activity was highly reversible as wash-out of aPPD resulted in an immediate recovery of P-gp activity. Unlike verapamil, aPPD did not affect ATPase activity of P-gp suggesting a different mechanism of action..
For research only, not for human use.
(20S)-Protopanaxadiol (20-Epiprotopanaxadiol) is an aglycon metabolic derivative of the protopanaxadiol-type ginseng saponin; apoptosis inducer.
Product Name: (20S)-Protopanaxadiol |cas: 30636-90-9 |cat number: DC9833 |Molecule Formular: C30H52O3 |MW: 460.73 |purity>98%
(20S)-Protopanaxadiol (20-Epiprotopanaxadiol) is an aglycon metabolic derivative of the protopanaxadiol-type ginseng saponin; apoptosis inducer.
Target: apoptosis inducer
(20S)-Protopanaxadiol was used to induce cytotoxicity for two human glioma cell lines, SF188 and U87MG. For the SF188 cells, (20S)-Protopanaxadiol activated caspases-3, -8, -7, and -9 within 3 h and induced rapid apoptosis, which could be partially inhibited by a general caspase blocker and completely abolished when the caspase blocker was used in combination with an antioxidant. (20S)-Protopanaxadiol also induced cell death in U87MG cells but did not activate any caspases in these cells [. aPPD was able to inhibit P-gp activity as potently as verapamil on MDR cells. The blockage of P-gp activity was highly reversible as wash-out of aPPD resulted in an immediate recovery of P-gp activity. Unlike verapamil, aPPD did not affect ATPase activity of P-gp suggesting a different mechanism of action..
For research only, not for human use.
Betulinic acid|cas 472-15-1|Supplied by DC Chem
Betulinic acid|cas 472-15-1|Supplied by DC Chem
Betulinic acid in stock,price: 450 USD/1g. Betulinic acid, a pentacyclic triterpene, selectively induces apoptosis in tumor cells, also is a inhibitor of HIV-1 with EC50 of 1.4 μ M.
Product Name: Betulinic acid |cas: 472-15-1 |cat number: DC9832 |Molecule Formular: C30H48O3 |MW: 456.7 |purity>98%
Betulinic acid, a pentacyclic triterpene, selectively induces apoptosis in tumor cells, also is a inhibitor of HIV-1 with EC50 of 1.4 μ M.
in vitro: Betulinic acid shows anti-HIV activity by blocking HIV replication in H9 lymphocytes with an EC50 value of 1.4 μM and inhibiting uninfected H9 cell growth with an IC50 value of 13 μM. Betulinic acid also acts as anti-melanoma agent through inhibiting aminopeptidase N activity with IC50 of 7.3 μM. In addition, Betulinic acid inhibits eukaryotic topoisomerase I activity with IC50 of 5 μM and can be exploited as a strong candidate for anti-tumor drug.
in vivo: Betulinic acid inhibits prostate cancer cell and tumor (xenograft) growth in athymic nude mice bearing LNCaP cells and this is due, in part, to proteasome-dependent downregulation of Sp1, Sp3, Sp4 and several Sp-regulated genes.
For research only, not for human use.
Betulinic acid in stock,price: 450 USD/1g. Betulinic acid, a pentacyclic triterpene, selectively induces apoptosis in tumor cells, also is a inhibitor of HIV-1 with EC50 of 1.4 μ M.
Product Name: Betulinic acid |cas: 472-15-1 |cat number: DC9832 |Molecule Formular: C30H48O3 |MW: 456.7 |purity>98%
Betulinic acid, a pentacyclic triterpene, selectively induces apoptosis in tumor cells, also is a inhibitor of HIV-1 with EC50 of 1.4 μ M.
in vitro: Betulinic acid shows anti-HIV activity by blocking HIV replication in H9 lymphocytes with an EC50 value of 1.4 μM and inhibiting uninfected H9 cell growth with an IC50 value of 13 μM. Betulinic acid also acts as anti-melanoma agent through inhibiting aminopeptidase N activity with IC50 of 7.3 μM. In addition, Betulinic acid inhibits eukaryotic topoisomerase I activity with IC50 of 5 μM and can be exploited as a strong candidate for anti-tumor drug.
in vivo: Betulinic acid inhibits prostate cancer cell and tumor (xenograft) growth in athymic nude mice bearing LNCaP cells and this is due, in part, to proteasome-dependent downregulation of Sp1, Sp3, Sp4 and several Sp-regulated genes.
For research only, not for human use.
GSK6853|GSK-6853|BRPF1 bromodomain inhibitor
GSK6853|GSK-6853|BRPF1 bromodomain inhibitor
GSK6853 is a potent, soluble, cell active, and highly selective inhibitor of the BRPF1 bromodomain
Product Name: GSK6853 |cas: 1910124-24-1 |cat number: DC9831 |Molecule Formular: C22H27N5O3 |MW: 409.21 |purity>98%
GSK6853 is a potent (300 pM), soluble, cell active (20 nM), and highly selective inhibitor of the BRPF1 bromodomain, and demonstrated properties suitable for cellular and in vivo studies.The BRPF (Bromodomain and PHD Finger-containing) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. A selective benzimidazolone BRPF1 inhibitor showing micromolar activity in a cellular target engagement assay was recently described.
For research only, not for human use.
GSK6853 is a potent, soluble, cell active, and highly selective inhibitor of the BRPF1 bromodomain
Product Name: GSK6853 |cas: 1910124-24-1 |cat number: DC9831 |Molecule Formular: C22H27N5O3 |MW: 409.21 |purity>98%
GSK6853 is a potent (300 pM), soluble, cell active (20 nM), and highly selective inhibitor of the BRPF1 bromodomain, and demonstrated properties suitable for cellular and in vivo studies.The BRPF (Bromodomain and PHD Finger-containing) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. A selective benzimidazolone BRPF1 inhibitor showing micromolar activity in a cellular target engagement assay was recently described.
For research only, not for human use.
AM-2394|AM2394|Glucokinase agonist (GKA)
AM-2394|AM2394|Glucokinase agonist (GKA)
AM-2394 in stock,550 USD/100mg. AM-2394 is a potent and selective Glucokinase agonist (GKA), which catalyzes the phosphorylation of glucose to glucose-6-phosphate.
Product Name: AM-2394 |cas: 1442684-77-6 |cat number: DC9830 |Molecule Formular: C22H25N5O4 |MW: 423.19 |purity>98%
AM-2394 is a potent and selective Glucokinase agonist (GKA), which catalyzes the phosphorylation of glucose to glucose-6-phosphate. AM-2394 activates GK with an EC50 of 60 nM, increases the affinity of GK for glucose by approximately 10-fold, exhibits moderate clearance and good oral bioavailability in multiple animal models, and lowers glucose excursion following an oral glucose tolerance test in an ob/ob mouse model of diabetes
For research only, not for human use.
AM-2394 in stock,550 USD/100mg. AM-2394 is a potent and selective Glucokinase agonist (GKA), which catalyzes the phosphorylation of glucose to glucose-6-phosphate.
Product Name: AM-2394 |cas: 1442684-77-6 |cat number: DC9830 |Molecule Formular: C22H25N5O4 |MW: 423.19 |purity>98%
AM-2394 is a potent and selective Glucokinase agonist (GKA), which catalyzes the phosphorylation of glucose to glucose-6-phosphate. AM-2394 activates GK with an EC50 of 60 nM, increases the affinity of GK for glucose by approximately 10-fold, exhibits moderate clearance and good oral bioavailability in multiple animal models, and lowers glucose excursion following an oral glucose tolerance test in an ob/ob mouse model of diabetes
For research only, not for human use.
IPI-549|IPI549|PI3K-gamma inhibitor
IPI-549|IPI549|PI3K-gamma inhibitor
IPI-549 in stock, 800 USD/100mg. IPI-549 is an orally administered immuno-oncology development candidate that selectively inhibits PI3K-gamma.
Product Name: IPI-549 |cas: N/A |cat number: DC9829 |Molecule Formular: C30H24N8O2 |MW: 528.2 |purity>98%
IPI-549 is an orally administered immuno-oncology development candidate that selectively inhibits PI3K-gamma. In preclinical studies, IPI-549 inhibits immune-suppressive macrophages within the tumor microenvironment, whereas other immunotherapies such as checkpoint modulators more directly target immune effector cell function. As such, IPI-549 may have the potential to treat a broad range of solid tumors and represents a potentially complementary approach to restoring anti-tumor immunity in combination with other immunotherapies such as checkpoint inhibitors.
For research only, not for human use.
IPI-549 in stock, 800 USD/100mg. IPI-549 is an orally administered immuno-oncology development candidate that selectively inhibits PI3K-gamma.
Product Name: IPI-549 |cas: N/A |cat number: DC9829 |Molecule Formular: C30H24N8O2 |MW: 528.2 |purity>98%
IPI-549 is an orally administered immuno-oncology development candidate that selectively inhibits PI3K-gamma. In preclinical studies, IPI-549 inhibits immune-suppressive macrophages within the tumor microenvironment, whereas other immunotherapies such as checkpoint modulators more directly target immune effector cell function. As such, IPI-549 may have the potential to treat a broad range of solid tumors and represents a potentially complementary approach to restoring anti-tumor immunity in combination with other immunotherapies such as checkpoint inhibitors.
For research only, not for human use.
YYA021|YYA-021|CD4 mimic anti-HIV activity
YYA021|YYA-021|CD4 mimic anti-HIV activity
YYA021 in stock, 500 USD/100mg. YYA-021 is a small-molecule CD4 mimic that inhibits HIV entry, with high anti-HIV activity and low cytotoxicity.
Product Name: YYA-021 |cas: 144217-65-2 |cat number: DC9828 |Molecule Formular: C18H27N3O2 |MW: 317.43 |purity>98%.
YYA-021 is a small-molecule CD4 mimic that inhibits HIV entry, with high anti-HIV activity and low cytotoxicity.
IC50 (=8.4 μM) value of YYA-021 is determined by a single round assay using cYTA48P virus and TZM-bl cells. YYA-021 is broadly distributed in tissues, probably as a result of its hydrophobicity. The plasma concentrations of YYA-021 in both species remained at micromolar levels for several hours post-injection.YYA-021 also enhances the neutralizing activity of KD-247 against simian-human immunodeficiency virus (SHIV)-KS661 strain via highly synergistic interactions. YYA-021 might have promise as a lead compound for the intravenous administration in a cocktail therapy with anti-gp120 monoclonal antibodies such as KD-247 and with co-receptor antagonists such as T140.
For research only, not for human use.
YYA021 in stock, 500 USD/100mg. YYA-021 is a small-molecule CD4 mimic that inhibits HIV entry, with high anti-HIV activity and low cytotoxicity.
Product Name: YYA-021 |cas: 144217-65-2 |cat number: DC9828 |Molecule Formular: C18H27N3O2 |MW: 317.43 |purity>98%.
YYA-021 is a small-molecule CD4 mimic that inhibits HIV entry, with high anti-HIV activity and low cytotoxicity.
IC50 (=8.4 μM) value of YYA-021 is determined by a single round assay using cYTA48P virus and TZM-bl cells. YYA-021 is broadly distributed in tissues, probably as a result of its hydrophobicity. The plasma concentrations of YYA-021 in both species remained at micromolar levels for several hours post-injection.YYA-021 also enhances the neutralizing activity of KD-247 against simian-human immunodeficiency virus (SHIV)-KS661 strain via highly synergistic interactions. YYA-021 might have promise as a lead compound for the intravenous administration in a cocktail therapy with anti-gp120 monoclonal antibodies such as KD-247 and with co-receptor antagonists such as T140.
For research only, not for human use.
AN3365|AN-3365|Epetraborole|antibiotic
AN3365|AN-3365|Epetraborole|antibiotic
AN3365(Epetraborole) in stock,price: 550 USD/100mg. AN3365 is a first-in-class antibiotic that demonstrates potent activity across a wide spectrum of Gram-negative bacteria, including those resistant to many other antibiotics.
Product Name: AN3365(Epetraborole) |cas: 1234563-16-6 |cat number: DC9827 |Molecule Formular: C11H16BNO4.HCl |MW: 273.52 |purity>98%
AN3365 is a novel boron-based, small-molecule product candidate that targets the bacterial enzyme leucyl tRNA synthetase. Preclinical studies suggest that AN3365 is a promising compound for the treatment of infections caused by a broad range of Gramnegative bacteria, including E. coli, K. pneumoniae, Citrobacter spp, S.marcescens, P.vulgaris, Providentia spp and Enterobacter spp. AN3365 has demonstrated a potent effect on strains harboring known resistance to widely-used antibiotics.
For research only, not for human use.
AN3365(Epetraborole) in stock,price: 550 USD/100mg. AN3365 is a first-in-class antibiotic that demonstrates potent activity across a wide spectrum of Gram-negative bacteria, including those resistant to many other antibiotics.
Product Name: AN3365(Epetraborole) |cas: 1234563-16-6 |cat number: DC9827 |Molecule Formular: C11H16BNO4.HCl |MW: 273.52 |purity>98%
AN3365 is a novel boron-based, small-molecule product candidate that targets the bacterial enzyme leucyl tRNA synthetase. Preclinical studies suggest that AN3365 is a promising compound for the treatment of infections caused by a broad range of Gramnegative bacteria, including E. coli, K. pneumoniae, Citrobacter spp, S.marcescens, P.vulgaris, Providentia spp and Enterobacter spp. AN3365 has demonstrated a potent effect on strains harboring known resistance to widely-used antibiotics.
For research only, not for human use.
BCTC|TRPM8 inhibitor
BCTC|TRPM8 inhibitor
BCTC in stock,price: 250 USD/100mg. BCTC is a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells.
Product Name: BCTC |cas: 393514-24-4 |cat number: DC9826 |Molecule Formular: C20H25ClN4O |MW: 372.89 |purity>98%
BCTC is a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells.
For research only, not for human use.
BCTC in stock,price: 250 USD/100mg. BCTC is a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells.
Product Name: BCTC |cas: 393514-24-4 |cat number: DC9826 |Molecule Formular: C20H25ClN4O |MW: 372.89 |purity>98%
BCTC is a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells.
For research only, not for human use.
Xanthohumol|COX inhibitor
Xanthohumol|COX inhibitor
Xanthohumol in stock,price: 250 USD/100mg. Xanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects.
Product Name: Xanthohumol |cas: 6754-58-1 |cat number: DC9825 |Molecule Formular: C21H22O5 |MW: 354.4 |purity>98%
Xanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects. Xanthohumol inhibits Cyp1A activity and induces QR activity in mouse hepatoma cell culture. Xanthohumol scavenges reactive oxygen species and inhibits superoxide anion radical and nitric oxide production. In addition, Xanthohumol prevents carcinogenesis via inhibition of DNA synthesis and induction of cell cycle arrest in S phase, apoptosis, and cell differentiation.Xanthohumol shows potent anti-HIV-1 activity.In CETP-Tg mice, xanthohumol (p.o.) prevents cholesterol accumulation leading to atherosclerosis. In TRAMP mice, xanthohumol (p.o.) induces a decrease in the average weight of the urogenital (UG) tract, delays advanced tumor progression and inhibits the growth of poorly differentiated prostate carcinoma.
For research only, not for human use.
Xanthohumol in stock,price: 250 USD/100mg. Xanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects.
Product Name: Xanthohumol |cas: 6754-58-1 |cat number: DC9825 |Molecule Formular: C21H22O5 |MW: 354.4 |purity>98%
Xanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects. Xanthohumol inhibits Cyp1A activity and induces QR activity in mouse hepatoma cell culture. Xanthohumol scavenges reactive oxygen species and inhibits superoxide anion radical and nitric oxide production. In addition, Xanthohumol prevents carcinogenesis via inhibition of DNA synthesis and induction of cell cycle arrest in S phase, apoptosis, and cell differentiation.Xanthohumol shows potent anti-HIV-1 activity.In CETP-Tg mice, xanthohumol (p.o.) prevents cholesterol accumulation leading to atherosclerosis. In TRAMP mice, xanthohumol (p.o.) induces a decrease in the average weight of the urogenital (UG) tract, delays advanced tumor progression and inhibits the growth of poorly differentiated prostate carcinoma.
For research only, not for human use.
Isosteviol|cas 27975-19-5
Isosteviol|cas 27975-19-5
Isosteviol in stock,price: 250 USD/100mg. Isosteviol is a derivative of stevioside, a constituent of Stevia rebaudiana, which is commonly used as a noncaloric sugar substitute in Japan and Brazil.
Product Name: Isosteviol |cas: 27975-19-5 |cat number: DC9824 |Molecule Formular: C20H30O3 |MW: 318.45 |purity>98%
Isosteviol dose-dependently relaxed the vasopressin (10-8 M)-induced vasoconstriction in isolated aortic rings with or without endothelium. However, in the presence of potassium chloride (3×10-2 M), the vasodilator effect of isosteviol on arterial strips disappeared. Only the inhibitors specific for the ATP-sensitive potassium (KATP) channel or small conductance calcium-activated potassium (SKCa) channel inhibited the vasodilator effect of isosteviol in isolated aortic rings contracted with 10-8 M vasopressin. The attenuation by isosteviol of the vasopressin- and phenylephrine-induced increase in [Ca (2+)]i was inhibited by glibenclamide, apamin and 4-aminopyridine but not by charybdotoxin. Furthermore, the inhibitory action of isosteviol on [Ca (2+)]i was blocked when A7r5 cells co-treated with glibenclamide and apamin in conjunction with 4-aminopyridine were present. Isosteviol (1-100 micromol/l) inhibits angiotensin-II-induced DNA synthesis and endothelin-1 secretion. Measurements of 2'7'-dichlorofluorescin diacetate, a redox-sensitive fluorescent dye, showed an isosteviol-mediated inhibition of intracellular reactive oxygen species generated by the effects of angiotensin II.
For research only, not for human use.
Isosteviol in stock,price: 250 USD/100mg. Isosteviol is a derivative of stevioside, a constituent of Stevia rebaudiana, which is commonly used as a noncaloric sugar substitute in Japan and Brazil.
Product Name: Isosteviol |cas: 27975-19-5 |cat number: DC9824 |Molecule Formular: C20H30O3 |MW: 318.45 |purity>98%
Isosteviol dose-dependently relaxed the vasopressin (10-8 M)-induced vasoconstriction in isolated aortic rings with or without endothelium. However, in the presence of potassium chloride (3×10-2 M), the vasodilator effect of isosteviol on arterial strips disappeared. Only the inhibitors specific for the ATP-sensitive potassium (KATP) channel or small conductance calcium-activated potassium (SKCa) channel inhibited the vasodilator effect of isosteviol in isolated aortic rings contracted with 10-8 M vasopressin. The attenuation by isosteviol of the vasopressin- and phenylephrine-induced increase in [Ca (2+)]i was inhibited by glibenclamide, apamin and 4-aminopyridine but not by charybdotoxin. Furthermore, the inhibitory action of isosteviol on [Ca (2+)]i was blocked when A7r5 cells co-treated with glibenclamide and apamin in conjunction with 4-aminopyridine were present. Isosteviol (1-100 micromol/l) inhibits angiotensin-II-induced DNA synthesis and endothelin-1 secretion. Measurements of 2'7'-dichlorofluorescin diacetate, a redox-sensitive fluorescent dye, showed an isosteviol-mediated inhibition of intracellular reactive oxygen species generated by the effects of angiotensin II.
For research only, not for human use.
Hederagenin|cas 465-99-6
Hederagenin|cas 465-99-6
Hederagenin in stock,price: 250 USD/100mg. Hederagenin a triterpenoid saponin, is used to study the properties of triterpenoid saponins as biopesticides that prevent fungal growth, bacterial growth, and viral plant diseases.
Product Name: Hederagenin |cas: 465-99-6 |cat number: DC9823 |Molecule Formular: C30H48O4 |MW: 472.7 |purity>98%
Hederagenin (3,23-Dihydroxyolean-12-en-28-acid), a triterpenoid saponin, is used to study the properties of triterpenoid saponins as biopesticides that prevent fungal growth, bacterial growth, and viral plant diseases. Hederagenin may be used as a reference in assays to detect it in biological fluids.
For research only, not for human use.
Hederagenin in stock,price: 250 USD/100mg. Hederagenin a triterpenoid saponin, is used to study the properties of triterpenoid saponins as biopesticides that prevent fungal growth, bacterial growth, and viral plant diseases.
Product Name: Hederagenin |cas: 465-99-6 |cat number: DC9823 |Molecule Formular: C30H48O4 |MW: 472.7 |purity>98%
Hederagenin (3,23-Dihydroxyolean-12-en-28-acid), a triterpenoid saponin, is used to study the properties of triterpenoid saponins as biopesticides that prevent fungal growth, bacterial growth, and viral plant diseases. Hederagenin may be used as a reference in assays to detect it in biological fluids.
For research only, not for human use.
EPZ020411|EPZ-020411|PRMT6 inhibitor|In stock
EPZ020411|EPZ-020411|PRMT6 inhibitor|In stock
EPZ020411 HCl in stock,price: 750 USD/100mg. EPZ020411 in stock, 750 USD/100mg. EPZ020411 is a potent and selective inhibitor of PRMT6 with IC50 of 10 nM, has ＞10 fold selectivity for PRMT6 over PRMT1 and PRMT8.
Product Name: EPZ020411 HCl |cas: 1700663-41-7 |cat number: DC9822 |Molecule Formular: C25H38N4O3.HCl |MW: 479.3 |purity>98%
EPZ020411 is a potent inhibitor of PRMT6 in biochemical (IC50 = 10 nM) and cellular (IC50 = 600 nM) assays. EPZ020411 is selective against the related enzymes PRMT3, PRMT4, PRMT5, and PRMT7 in a biochemical assay, and relatively selective against PRMT1 and PRMT8. In biochemical (IC50s = 100 and 200 nM, respectively) and cellular assays (for PRMT1). Even though EPZ020411 is selective within the PRMT family, there is no information on other relevant human methyltransferases.EPZ020411 is not greatly selective for PRMT6 over PRMT1 or PRMT8 in vitro. PRMT6 is the only PRMT known to methylate the H3R2 position, and EPZ020411 can be used as a probe to assess the functionality of this post-translational modification. While this compound shows poor bioavailability following oral dosing (<5%), subcutaneous (SC) dosing results in significant plasma levels, making this compound suitable for in vivo studies of the H3R2 mark using SC dosing.
For research only, not for human use.
EPZ020411 HCl in stock,price: 750 USD/100mg. EPZ020411 in stock, 750 USD/100mg. EPZ020411 is a potent and selective inhibitor of PRMT6 with IC50 of 10 nM, has ＞10 fold selectivity for PRMT6 over PRMT1 and PRMT8.
Product Name: EPZ020411 HCl |cas: 1700663-41-7 |cat number: DC9822 |Molecule Formular: C25H38N4O3.HCl |MW: 479.3 |purity>98%
EPZ020411 is a potent inhibitor of PRMT6 in biochemical (IC50 = 10 nM) and cellular (IC50 = 600 nM) assays. EPZ020411 is selective against the related enzymes PRMT3, PRMT4, PRMT5, and PRMT7 in a biochemical assay, and relatively selective against PRMT1 and PRMT8. In biochemical (IC50s = 100 and 200 nM, respectively) and cellular assays (for PRMT1). Even though EPZ020411 is selective within the PRMT family, there is no information on other relevant human methyltransferases.EPZ020411 is not greatly selective for PRMT6 over PRMT1 or PRMT8 in vitro. PRMT6 is the only PRMT known to methylate the H3R2 position, and EPZ020411 can be used as a probe to assess the functionality of this post-translational modification. While this compound shows poor bioavailability following oral dosing (<5%), subcutaneous (SC) dosing results in significant plasma levels, making this compound suitable for in vivo studies of the H3R2 mark using SC dosing.
For research only, not for human use.
Ezutromid|utrophin's translation modulator
Ezutromid|utrophin's translation modulator
Ezutromid in stock,price: 500 USD/100mg. Ezutromid is a novel Small utrophin's translation modulator with EC50 of 0.4 uM .
Product Name: Ezutromid |cas: 945531-77-1 |cat number: DC9821 |Molecule Formular: C19H15NO3S |MW: 337.39 |purity>98%
Ezutromid is a novel Small utrophin's translation modulator with EC50 of 0.4 uM .
In vitro: 1) SMT C1100 induces increased levels of utrophin RNA in human muscle cells.
2) Treatment of human DMD cells with SMT C1100 lead to a 2-fold increase in utrophin protein levels at an optimal concentration of 0.3 uM after 3 days of treatment.
3) SMT C1100 wassafe and well tolerated with plasma concentrations achieved suf?cient to cause a 50% increase in concentrations of utrophin in cells.
4) SMT C1100 led to a 30% increase in Utrn mRNA level and resulted in a 2.0-fold increase in UTRN protein level .
In vivo: 1)The reference for administration is 50 mg/kg.
2) it was considered that no toxicity was determined for SMT C1100 administered by oral gavage to the mouse up to dose levels of 2000 mg/kg/day for 28 days.
For research only, not for human use.
Ezutromid in stock,price: 500 USD/100mg. Ezutromid is a novel Small utrophin's translation modulator with EC50 of 0.4 uM .
Product Name: Ezutromid |cas: 945531-77-1 |cat number: DC9821 |Molecule Formular: C19H15NO3S |MW: 337.39 |purity>98%
Ezutromid is a novel Small utrophin's translation modulator with EC50 of 0.4 uM .
In vitro: 1) SMT C1100 induces increased levels of utrophin RNA in human muscle cells.
2) Treatment of human DMD cells with SMT C1100 lead to a 2-fold increase in utrophin protein levels at an optimal concentration of 0.3 uM after 3 days of treatment.
3) SMT C1100 wassafe and well tolerated with plasma concentrations achieved suf?cient to cause a 50% increase in concentrations of utrophin in cells.
4) SMT C1100 led to a 30% increase in Utrn mRNA level and resulted in a 2.0-fold increase in UTRN protein level .
In vivo: 1)The reference for administration is 50 mg/kg.
2) it was considered that no toxicity was determined for SMT C1100 administered by oral gavage to the mouse up to dose levels of 2000 mg/kg/day for 28 days.
For research only, not for human use.
ML-281|ML281|STK33 inhibitor
ML-281|ML281|STK33 inhibitor
ML281 in stock,price: 550 USD/100mg. ML281 is a potent and selective STK33 inhibitor with IC50 of 14 nM. ML281 showed a 550-fold selectivity over AurB and greater than 700-fold selectivity over PKA.
Product Name: ML281 |cas: 1404437-62-2 |cat number: DC9820 |Molecule Formular: C22H19N3O2S |MW: 389.47 |purity>98%
ML281 is a potent and selective STK33 inhibitor with IC50 of 14 nM. ML281 showed a 550-fold selectivity over AurB and greater than 700-fold selectivity over PKA.ML281 showed low nanomolar inhibition of purified recombinant STK33 and a distinct selectivity profile as compared to other STK33 inhibitors. Even at the highest concentration tested (10 μM), ML281 had no effect on the viability of KRAS-dependent cancer cells.
For research only, not for human use.
ML281 in stock,price: 550 USD/100mg. ML281 is a potent and selective STK33 inhibitor with IC50 of 14 nM. ML281 showed a 550-fold selectivity over AurB and greater than 700-fold selectivity over PKA.
Product Name: ML281 |cas: 1404437-62-2 |cat number: DC9820 |Molecule Formular: C22H19N3O2S |MW: 389.47 |purity>98%
ML281 is a potent and selective STK33 inhibitor with IC50 of 14 nM. ML281 showed a 550-fold selectivity over AurB and greater than 700-fold selectivity over PKA.ML281 showed low nanomolar inhibition of purified recombinant STK33 and a distinct selectivity profile as compared to other STK33 inhibitors. Even at the highest concentration tested (10 μM), ML281 had no effect on the viability of KRAS-dependent cancer cells.
For research only, not for human use.
Guanoclor|cas 5001-32-1
Guanoclor|cas 5001-32-1
Guanoclor in stock,price:450 USD/1G. Guanoclor is a sympatholytic drug. It is known to bind to non-adrenergic sites in pig kidney membranes.
Product Name: Guanoclor |cas: 5001-32-1 |cat number: DC9819 |Molecule Formular: C9H12Cl2N4O |MW: 263.12 |purity>98%
For research only, not for human use.
Guanoclor in stock,price:450 USD/1G. Guanoclor is a sympatholytic drug. It is known to bind to non-adrenergic sites in pig kidney membranes.
Product Name: Guanoclor |cas: 5001-32-1 |cat number: DC9819 |Molecule Formular: C9H12Cl2N4O |MW: 263.12 |purity>98%
For research only, not for human use.
Azoramide|unfolded protein response (UPR)Modulator
Azoramide|unfolded protein response (UPR)Modulator
Azoramide in stock,price: 300 USD/100mg. Azoramide is a small-molecule modulator of the unfolded protein response with antidiabetic activity.
Product Name: Azoramide |cas: 932986-18-0 |cat number: DC9818 |Molecule Formular: C15H17ClN2OS |MW: 308.83 |purity>98%
Azoramide is a small-molecule modulator of the unfolded protein response with antidiabetic activity.
For research only, not for human use.
Azoramide in stock,price: 300 USD/100mg. Azoramide is a small-molecule modulator of the unfolded protein response with antidiabetic activity.
Product Name: Azoramide |cas: 932986-18-0 |cat number: DC9818 |Molecule Formular: C15H17ClN2OS |MW: 308.83 |purity>98%
Azoramide is a small-molecule modulator of the unfolded protein response with antidiabetic activity.
For research only, not for human use.
Necrosulfonamide (NSA)|necrosis inhibitor
Necrosulfonamide (NSA)|necrosis inhibitor
Necrosulfonamide (NSA) in stock,price: 300 USD/100mg. Necrosulfonamide (NSA) is a very specific and potent necrosis inhibitor with an IC50 less than 0.2 uM.
Product Name: Necrosulfonamide (NSA) |cas: 1360614-48-7 |cat number: DC9817 |Molecule Formular: C18H15N5O6S2 |MW: 461.47 |purity>98%
Necrosulfonamide (NSA) is a very specific and potent necrosis inhibitor with an IC50 less than 0.2 uM. It specifically blocks necrosis downstream of receptor-interacting serine-threonine kinase 3 (RIP3) activation. RIP3 is a key signaling molecule in the programmed necrosis pathway. Treating cells with NSA arrested necrosis at a specific step at which RIP3 formed discrete punctae in cells. Different from Necrostatin-1, NSA does not inhibit the necrosis-induced RIP1 and RIP3 interactions. NSA targets MLKL, a critical substrate of RIP3 during induction of necrosis. It binds the N-terminal of MLKL, covalently modifies Cys86 of human MLKL, and prevents necrosome from interacting with its downstream effectors.
For research only, not for human use.
Necrosulfonamide (NSA) in stock,price: 300 USD/100mg. Necrosulfonamide (NSA) is a very specific and potent necrosis inhibitor with an IC50 less than 0.2 uM.
Product Name: Necrosulfonamide (NSA) |cas: 1360614-48-7 |cat number: DC9817 |Molecule Formular: C18H15N5O6S2 |MW: 461.47 |purity>98%
Necrosulfonamide (NSA) is a very specific and potent necrosis inhibitor with an IC50 less than 0.2 uM. It specifically blocks necrosis downstream of receptor-interacting serine-threonine kinase 3 (RIP3) activation. RIP3 is a key signaling molecule in the programmed necrosis pathway. Treating cells with NSA arrested necrosis at a specific step at which RIP3 formed discrete punctae in cells. Different from Necrostatin-1, NSA does not inhibit the necrosis-induced RIP1 and RIP3 interactions. NSA targets MLKL, a critical substrate of RIP3 during induction of necrosis. It binds the N-terminal of MLKL, covalently modifies Cys86 of human MLKL, and prevents necrosome from interacting with its downstream effectors.
For research only, not for human use.
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