SAGE-217|SAGE217|cas 1632051-40-1
DC Chemicals, Website:www.dcchemicals.com
Product Name: SAGE-217|CAS: 1632051-40-1|Cat No: DC10802|Other Names: SAGE-217; SAGE 217; SAGE217,1632051-40-1
SAGE-217 is a potent GABAA receptor agonist with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively.
Kinase assay demonstrates that SAGE-217 is a potent GABAA receptor agonist with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively. SAGE-217 is currently being studied in parallel phase 2 clinical trials for the treatment of postpartum depression (PPD) and major depressive disorder (MDD). SAGE-217 shows >30 μM inhibition in a cardiac panel of eight relevant cardiac ion channels. At 10 μM concentration of SAGE-217, only binding at the glycine (57%), sigma receptors (88%), and inhibition of the transient receptor potential vanilloid 1 (TRPV1, 95%) is noted.Acute administration of SAGE-217 (0.3 to 10 mg/kg, ip) effectively reduces pentylenetretazol (PTZ)-induced seizures in mice (MECplasma=85 nM) as well as produces a dose-dependent anticonvulsant effect in the mouse 6 Hz electrical stimulation model. In the rat lithium-pilocarpine model of status epilepticus (SE), SAGE-217 (0.3 to 5 mg, iv) abolishes both behavioral and electrographic seizure activity, even when administered 60 min after induction of SE. Additional PK studies of SAGE-217 in dog show low clearance (<10% of hepatic blood flow), resulting in excellent oral bioavailability (F=68%).
2018年5月18日星期五
AMPA/kainate antagonist-2
AMPA/kainate antagonist-2
DC Chemicals, Website:www.dcchemicals.com
Product Name: AMPA/kainate antagonist-2|CAS: 923271-87-8|Cat No: DC10801|Other Names:
A novel Non-competitive AMPA/kainate antagonist.
DC Chemicals, Website:www.dcchemicals.com
Product Name: AMPA/kainate antagonist-2|CAS: 923271-87-8|Cat No: DC10801|Other Names:
A novel Non-competitive AMPA/kainate antagonist.
AMPA/kainate antagonist-1
AMPA/kainate antagonist-1
DC Chemicals, Website:www.dcchemicals.com
Product Name: AMPA/kainate antagonist-1|CAS: 732277-05-3|Cat No: DC10800|Other Names:
A novel Non-competitive AMPA/kainate antagonist.
DC Chemicals, Website:www.dcchemicals.com
Product Name: AMPA/kainate antagonist-1|CAS: 732277-05-3|Cat No: DC10800|Other Names:
A novel Non-competitive AMPA/kainate antagonist.
D-Lin-MC3-DMA|for siRNA delivery|Supplier
D-Lin-MC3-DMA|for siRNA delivery|Supplier
DC Chemicals, Website:www.dcchemicals.com
Product Name: DLin-MC3-DMA|CAS: N/A|Cat No: DC10800|Other Names: D-Lin-MC3-DMA,DLinMC3DMA,D-Lin-MC-3-DMA,D-Lin-MC3-DMA
D-Lin-MC3-DMA(MC3) is the most potent cationic lipid that has been synthesized for Lipid nanoparticles (LNPs) to deliver the siRNA.
Technological advances in both siRNA (small interfering RNA) and whole genome sequencing have demonstrated great potential in translating genetic information into siRNA-based drugs to halt the synthesis of most disease-causing proteins. Despite its powerful promises as a drug, siRNA requires a sophisticated delivery vehicle because of its rapid degradation in the circulation, inefficient accumulation in target tissues and inability to cross cell membranes to access the cytoplasm where it functions. Lipid nanoparticle (LNP) containing ionizable amino lipids is the leading delivery technology for siRNA, with five products in clinical trials and more in the pipeline. Lipid nanoparticles (LNPs) formed by an ionizable cationic lipid (DLin-MC3-DMA), helper lipids (distearoylphosphatidylcholine, DSPC, and cholesterol), and a poly(ethylene glycol) (PEG) lipid have been identified as very promising delivery vectors of short interfering RNA (siRNA) in different clinical phases. DLin-MC3-DMA [14], which are 100-fold and 1000-fold more potent, respectively, in silencing of a hepatic gene (Factor VII) in comparison to the previous generation lipid DLin-DMA (1,2-dilinoleyloxy-N,N-dimethyl-3-aminopropane).The ED50 (median effective dose) for LNP containing DLin-MC3-DMA to silence Factor VII in mice and TTR in non-human primates was 0.005 mg/kg and 0.03 mg/kg, respectively. One of the key findings from these studies was the optimum lipid pKa value of 6.2–6.5 as a dominating factor in determining hepatic gene-silencing activity in vivo. DLin-MC3-DMA, having a pKa of 6.44, is currently the most active ionizable lipid being used in clinical trials.
DC Chemicals, Website:www.dcchemicals.com
Product Name: DLin-MC3-DMA|CAS: N/A|Cat No: DC10800|Other Names: D-Lin-MC3-DMA,DLinMC3DMA,D-Lin-MC-3-DMA,D-Lin-MC3-DMA
D-Lin-MC3-DMA(MC3) is the most potent cationic lipid that has been synthesized for Lipid nanoparticles (LNPs) to deliver the siRNA.
Technological advances in both siRNA (small interfering RNA) and whole genome sequencing have demonstrated great potential in translating genetic information into siRNA-based drugs to halt the synthesis of most disease-causing proteins. Despite its powerful promises as a drug, siRNA requires a sophisticated delivery vehicle because of its rapid degradation in the circulation, inefficient accumulation in target tissues and inability to cross cell membranes to access the cytoplasm where it functions. Lipid nanoparticle (LNP) containing ionizable amino lipids is the leading delivery technology for siRNA, with five products in clinical trials and more in the pipeline. Lipid nanoparticles (LNPs) formed by an ionizable cationic lipid (DLin-MC3-DMA), helper lipids (distearoylphosphatidylcholine, DSPC, and cholesterol), and a poly(ethylene glycol) (PEG) lipid have been identified as very promising delivery vectors of short interfering RNA (siRNA) in different clinical phases. DLin-MC3-DMA [14], which are 100-fold and 1000-fold more potent, respectively, in silencing of a hepatic gene (Factor VII) in comparison to the previous generation lipid DLin-DMA (1,2-dilinoleyloxy-N,N-dimethyl-3-aminopropane).The ED50 (median effective dose) for LNP containing DLin-MC3-DMA to silence Factor VII in mice and TTR in non-human primates was 0.005 mg/kg and 0.03 mg/kg, respectively. One of the key findings from these studies was the optimum lipid pKa value of 6.2–6.5 as a dominating factor in determining hepatic gene-silencing activity in vivo. DLin-MC3-DMA, having a pKa of 6.44, is currently the most active ionizable lipid being used in clinical trials.
SSR-240612|SSR240612|cas 464930-42-5
SSR-240612|SSR240612|cas 464930-42-5
DC Chemicals, Website:www.dcchemicals.com
Product Name: SSR-240612 HCl |CAS: 464930-42-5|Cat No: DC10799|Other Names: SSR-240612; SSR240612; SSR 240612
SSR-240612 is a bradykinin B1 receptor antagonist potentially for the treatment of chronic pain.
SSR240612 blocked tactile and cold allodynia at 3h (ID50=5.5and 7.1mg/kg,respectively) in glucose‐fed rats but had no effect in control rats. The antagonist (10mg/kg) had no effect on plasma glucose and insulin, insulin resistance (HOMA index) and aortic superoxide anion production in glucose-fed rats.
DC Chemicals, Website:www.dcchemicals.com
Product Name: SSR-240612 HCl |CAS: 464930-42-5|Cat No: DC10799|Other Names: SSR-240612; SSR240612; SSR 240612
SSR-240612 is a bradykinin B1 receptor antagonist potentially for the treatment of chronic pain.
SSR240612 blocked tactile and cold allodynia at 3h (ID50=5.5and 7.1mg/kg,respectively) in glucose‐fed rats but had no effect in control rats. The antagonist (10mg/kg) had no effect on plasma glucose and insulin, insulin resistance (HOMA index) and aortic superoxide anion production in glucose-fed rats.
p38-α MAPK-IN-1 |MAPK14 inhibitor|443913-15-3
p38-α MAPK-IN-1 |MAPK14 inhibitor|443913-15-3
DC Chemicals, Website:www.dcchemicals.com
Product Name: p38-α MAPK-IN-1|CAS: 443913-15-3|Cat No: DC10798|Other Names: MAPK14 inhibitor
p38-α MAPK-IN-1 is an inhibitor of MAPK14 (p38-α), with IC50 of 2300 nM in EFC displacement assay, and 5500 nM in HTRF assay.
DC Chemicals, Website:www.dcchemicals.com
Product Name: p38-α MAPK-IN-1|CAS: 443913-15-3|Cat No: DC10798|Other Names: MAPK14 inhibitor
p38-α MAPK-IN-1 is an inhibitor of MAPK14 (p38-α), with IC50 of 2300 nM in EFC displacement assay, and 5500 nM in HTRF assay.
AB423|AB-423||Hepatitis B Virus Capsid Assembly inhibitor
AB423|AB-423||Hepatitis B Virus Capsid Assembly inhibitor
DC Chemicals, Website:www.dcchemicals.com
Product Name: AB423|CAS: 1572510-80-5|Cat No: DC10797|Other Names: AB423,AB-423,AB 423
AB-423 is the first-generation Hepatitis B Virus Capsid Assembly inhibitor, which was generally safe and well tolerated in Phase 1 healthy volunteer studies.
AB-423 is a potent, highly seletive inhibitor of HBV replication through a block of pgRNA encapsidation. AB-423 in combination with EVT has shown synergistic antiviral activity in vitro in primary human hepatocytes. Furthermore, AB-423 alone and in combination with entecavir has shown potent in vivo activity in a hydrodynamic injection (HDI) mouse model of HBV.The HBV capsid inhibitor AB-423 exhibits a dual mode of inhibition:inhibited encapsidation of pgRNA during ongoing infection; inhibited cccDNA synthesis presumably via inhibition of the capsid uncoating step.In vitro AB-423 showed: pan-genotypic activity; potent activity against HBV in combination with Nucs, IFN, and RNAi agents;no significant activity against unrelated viruses.
DC Chemicals, Website:www.dcchemicals.com
Product Name: AB423|CAS: 1572510-80-5|Cat No: DC10797|Other Names: AB423,AB-423,AB 423
AB-423 is the first-generation Hepatitis B Virus Capsid Assembly inhibitor, which was generally safe and well tolerated in Phase 1 healthy volunteer studies.
AB-423 is a potent, highly seletive inhibitor of HBV replication through a block of pgRNA encapsidation. AB-423 in combination with EVT has shown synergistic antiviral activity in vitro in primary human hepatocytes. Furthermore, AB-423 alone and in combination with entecavir has shown potent in vivo activity in a hydrodynamic injection (HDI) mouse model of HBV.The HBV capsid inhibitor AB-423 exhibits a dual mode of inhibition:inhibited encapsidation of pgRNA during ongoing infection; inhibited cccDNA synthesis presumably via inhibition of the capsid uncoating step.In vitro AB-423 showed: pan-genotypic activity; potent activity against HBV in combination with Nucs, IFN, and RNAi agents;no significant activity against unrelated viruses.
Prexasertib (LY2606368)|LY 2606368|DC Chemicals
Prexasertib (LY2606368)|LY 2606368|DC Chemicals
DC Chemicals, Website:www.dcchemicals.com
Product Name: Prexasertib (LY2606368) |CAS: 1234015-52-1|Cat No: DC10796|Other Names: LY 2606368,LY-2606368
LY2606368 is a potent and selective ATP competitive inhibitor(IC50=1.5 nM in SW1990 cell) of the Chk1 protein kinase.
LY2606368 is a potent and selective ATP competitive inhibitor(IC50=1.5 nM in SW1990 cell) of the Chk1 protein kinase.LY2606368 alone significantly inhibited the cell proliferation in a variety of pancreatic cell lines (SW1990, SU86.86, Bx-PC3, AsPC-1, CFPAC-1, Capan-2, HPAF-II) with SW1990 being the most sensitive (IC50=1.5 nM).
LY2606368 has been reported to inhibit Chk1 auto-phosphorylation activated by DNA damaging agents, and induce phosphorylation of H2AX, a DNA damage maker in multiple cancer cell lines in vitro. In addition, LY2606368 has demonstrated potent single agent activity and potentiates the anti-tumor activity of DNA damaging agents in vivo. Pancreatic cancer is one of the least curable cancers, with an approximate 5% overall 5-year survival for all patients. In SW1990 pancreas orthotopic model, which represents the local and metastatic growth pattern seen in pancreas cancer patients, LY2606368 treatment resulted in over 92% inhibition of primary tumor growth as well as 100% inhibition of metastasis to lymph node, spleen and intestine. The anti-tumor effect of LY2606368 treatment was further demonstrated in comparing with gemcitabine (the standard of care for pancreas cancer patient) in SW1990 orthotopic model. For the detailed information of LY2606368 dihydrochloride, the solubility of LY2606368 dihydrochloride in water, the solubility of LY2606368 dihydrochloride in DMSO, the solubility of LY2606368 dihydrochloride in PBS buffer, the animal experiment (test) of LY2606368 dihydrochloride, the cell expriment (test) of LY2606368 dihydrochloride, the in vivo, in vitro and clinical trial test of LY2606368 dihydrochloride, the EC50, IC50,and affinity,of LY2606368 dihydrochloride, Please contact DC Chemicals.
DC Chemicals, Website:www.dcchemicals.com
Product Name: Prexasertib (LY2606368) |CAS: 1234015-52-1|Cat No: DC10796|Other Names: LY 2606368,LY-2606368
LY2606368 is a potent and selective ATP competitive inhibitor(IC50=1.5 nM in SW1990 cell) of the Chk1 protein kinase.
LY2606368 is a potent and selective ATP competitive inhibitor(IC50=1.5 nM in SW1990 cell) of the Chk1 protein kinase.LY2606368 alone significantly inhibited the cell proliferation in a variety of pancreatic cell lines (SW1990, SU86.86, Bx-PC3, AsPC-1, CFPAC-1, Capan-2, HPAF-II) with SW1990 being the most sensitive (IC50=1.5 nM).
LY2606368 has been reported to inhibit Chk1 auto-phosphorylation activated by DNA damaging agents, and induce phosphorylation of H2AX, a DNA damage maker in multiple cancer cell lines in vitro. In addition, LY2606368 has demonstrated potent single agent activity and potentiates the anti-tumor activity of DNA damaging agents in vivo. Pancreatic cancer is one of the least curable cancers, with an approximate 5% overall 5-year survival for all patients. In SW1990 pancreas orthotopic model, which represents the local and metastatic growth pattern seen in pancreas cancer patients, LY2606368 treatment resulted in over 92% inhibition of primary tumor growth as well as 100% inhibition of metastasis to lymph node, spleen and intestine. The anti-tumor effect of LY2606368 treatment was further demonstrated in comparing with gemcitabine (the standard of care for pancreas cancer patient) in SW1990 orthotopic model. For the detailed information of LY2606368 dihydrochloride, the solubility of LY2606368 dihydrochloride in water, the solubility of LY2606368 dihydrochloride in DMSO, the solubility of LY2606368 dihydrochloride in PBS buffer, the animal experiment (test) of LY2606368 dihydrochloride, the cell expriment (test) of LY2606368 dihydrochloride, the in vivo, in vitro and clinical trial test of LY2606368 dihydrochloride, the EC50, IC50,and affinity,of LY2606368 dihydrochloride, Please contact DC Chemicals.
CM-272|CM272|CAS 1846570-31-7
CM-272|CM272|CAS 1846570-31-7
DC Chemicals, Website:www.dcchemicals.com
Product Name: CM-272|CAS: 1846570-31-7|Cat No: DC10795|Other Names: CM-272; CM 272; CM272
CM-272 is a first-in-class reversible dual small molecule inhibitor against G9a and DNMTs in hematological malignancies.
CM-272 is a first-in-class reversible and substrate-competitive dual inhibitor of G9a and DNMTs. In ALL, AML and DLBCL-derived cell lines, CM-272 reduced DNA methylation in the promoter region of specific tumor suppressor genes. CM-272 also inhibited cell proliferation, blocked cell cycle progression and induced apoptosis in a dose-dependent way.
DC Chemicals, Website:www.dcchemicals.com
Product Name: CM-272|CAS: 1846570-31-7|Cat No: DC10795|Other Names: CM-272; CM 272; CM272
CM-272 is a first-in-class reversible dual small molecule inhibitor against G9a and DNMTs in hematological malignancies.
CM-272 is a first-in-class reversible and substrate-competitive dual inhibitor of G9a and DNMTs. In ALL, AML and DLBCL-derived cell lines, CM-272 reduced DNA methylation in the promoter region of specific tumor suppressor genes. CM-272 also inhibited cell proliferation, blocked cell cycle progression and induced apoptosis in a dose-dependent way.
PH-002,PH002|AD treament|apo E4 inhibitor
PH-002,PH002|AD treament|apo E4 inhibitor
DC Chemicals, Website:www.dcchemicals.com
Product Name: PH-002|CAS: 1311174-68-1|Cat No: DC10794|Other Names: PH002,PH-002,PH 002
PH-002 is a small-molecule structure corrector,inhibitor of apolipoprotein (apo) E4 intramolecular domain interaction,a potent candidate drug for the treament of AD(Alzheimer disease)
PH-002 is an inhibitor of apolipoprotein (apo) E4 intramolecular domain interaction in neuronal cells that restores mitochondrial cytochrome c oxidase subunit 1 levels, rescues impairments of mitochondrial motility and neurite outgrowth. PH-002 is an apoE4 structure corrector that reverses the apoE4 detrimental effects. The researchers confirmed that, in human neurons, the misshapen apoE4 protein cannot function properly and is broken down into disease-causing fragments in the cells. This process results in a number of problems commonly found in Alzheimer's disease, including the accumulation of the protein tau and of amyloid peptides.
DC Chemicals, Website:www.dcchemicals.com
Product Name: PH-002|CAS: 1311174-68-1|Cat No: DC10794|Other Names: PH002,PH-002,PH 002
PH-002 is a small-molecule structure corrector,inhibitor of apolipoprotein (apo) E4 intramolecular domain interaction,a potent candidate drug for the treament of AD(Alzheimer disease)
PH-002 is an inhibitor of apolipoprotein (apo) E4 intramolecular domain interaction in neuronal cells that restores mitochondrial cytochrome c oxidase subunit 1 levels, rescues impairments of mitochondrial motility and neurite outgrowth. PH-002 is an apoE4 structure corrector that reverses the apoE4 detrimental effects. The researchers confirmed that, in human neurons, the misshapen apoE4 protein cannot function properly and is broken down into disease-causing fragments in the cells. This process results in a number of problems commonly found in Alzheimer's disease, including the accumulation of the protein tau and of amyloid peptides.
ML 221|ML221|CAS 877636-42-5
ML 221|ML221|CAS 877636-42-5
DC Chemicals, Website:www.dcchemicals.com
Product Name: ML221|CAS: 877636-42-5|Cat No: DC10793|Other Names: ML221; ML 221; ML-221
ML221 is an antagonist of the apelin (APJ) receptor.
Apelin receptor (APJ) antagonist (IC50 values are 0.70 and 1.75 μM in a cAMP assay and β-arrestin assay, respectively). Displays >37-fold selectivity over the closely related angiotensin II type 1 (AT1) receptor. Exhibits no toxicity towards human hepatocytes at concentrations >50 μM.
DC Chemicals, Website:www.dcchemicals.com
Product Name: ML221|CAS: 877636-42-5|Cat No: DC10793|Other Names: ML221; ML 221; ML-221
ML221 is an antagonist of the apelin (APJ) receptor.
Apelin receptor (APJ) antagonist (IC50 values are 0.70 and 1.75 μM in a cAMP assay and β-arrestin assay, respectively). Displays >37-fold selectivity over the closely related angiotensin II type 1 (AT1) receptor. Exhibits no toxicity towards human hepatocytes at concentrations >50 μM.
DIM-C-pPhOCH3(C-DIM5)|Nur77 antagonist|CAS 151358-47-3
DIM-C-pPhOCH3(C-DIM5)|Nur77 antagonist|CAS 151358-47-3
DC Chemicals, Website:www.dcchemicals.com
Product Name: DIM-C-pPhOCH3(C-DIM5)|CAS: 33985-68-1|Cat No: DC10792|Other Names:
C-DIM5 is a Nur77 agonist. Activation of the orphan nuclear receptor Nur77 by C-DIM5 is associated with decreased cancer cell survival,
C-DIM5 is a Nur77 agonist. Activation of the orphan nuclear receptor Nur77 by C-DIM5 is associated with decreased cancer cell survival, induction of apoptosis, induced expression of the apoptosis gene/protein TRAIL, and inhibited tumor growth in vivo. C-DIM5 induces G0-G1–phase to S-phase arrest in Panc1 cells, and this is accompanied by Nur77-dependent induction of the cyclin-dependent kinase inhibitor p21.
DC Chemicals, Website:www.dcchemicals.com
Product Name: DIM-C-pPhOCH3(C-DIM5)|CAS: 33985-68-1|Cat No: DC10792|Other Names:
C-DIM5 is a Nur77 agonist. Activation of the orphan nuclear receptor Nur77 by C-DIM5 is associated with decreased cancer cell survival,
C-DIM5 is a Nur77 agonist. Activation of the orphan nuclear receptor Nur77 by C-DIM5 is associated with decreased cancer cell survival, induction of apoptosis, induced expression of the apoptosis gene/protein TRAIL, and inhibited tumor growth in vivo. C-DIM5 induces G0-G1–phase to S-phase arrest in Panc1 cells, and this is accompanied by Nur77-dependent induction of the cyclin-dependent kinase inhibitor p21.
DIM-C-pPhOH(CDIM8)|Nur77 antagonist|CAS 151358-47-3
DIM-C-pPhOH(CDIM8)|Nur77 antagonist|CAS 151358-47-3
DC Chemicals, Website:www.dcchemicals.com
Product Name: DIM-C-pPhOH(CDIM8)|CAS: 151358-47-3|Cat No: DC10791|Other Names:
DIM-C-pPhOH is a Nur77 Antagonist. DIM-C-pPhOH inhibits lung cancer cell and tumor growth in a metastasis model.
Nur77 (NR4A1) antagonist. Inhibits TGF-β induced cell migration of breast cancer cell lines. Promotes ROS/endoplasmic reticulum stress and proapoptotic pathways in pancreatic cancer cell lines. Mimics effects of Nur77 RNAi silencing.
DC Chemicals, Website:www.dcchemicals.com
Product Name: DIM-C-pPhOH(CDIM8)|CAS: 151358-47-3|Cat No: DC10791|Other Names:
DIM-C-pPhOH is a Nur77 Antagonist. DIM-C-pPhOH inhibits lung cancer cell and tumor growth in a metastasis model.
Nur77 (NR4A1) antagonist. Inhibits TGF-β induced cell migration of breast cancer cell lines. Promotes ROS/endoplasmic reticulum stress and proapoptotic pathways in pancreatic cancer cell lines. Mimics effects of Nur77 RNAi silencing.
ML-239|ML239|CAS 1378872-36-6
ML-239|ML239|CAS 1378872-36-6
DC Chemicals, Website:www.dcchemicals.com
Product Name: ML-239|CAS: 1378872-36-6|Cat No: DC10790|Other Names: CID-49843203,CID 49843203,CID49843203,ML-239,ML 239,ML239,1378872-36-6
ML-239 is an inhibitor of cancer stem cells, displaying greater than 23-fold selective inhibition of a breast cancer stem cell-like cell line (EC50 = 1.18 µM) over an isogenic control cell line (EC50 = 27.6 µM).
ML239 (Compound 7j) is a potent and selective inhibitor of breast cancer stem cells, with an IC50 of 1.16 μM, with ∼24-fold selectivity against the control cell line. ML239 inhibits breast cancer stem-like cells, most likely through activation of fatty acid desaturase 2 (FADS2). ML239 is cytotoxic to NCIH661 cells, and FADS2 knockdown reduces ML239 cytotoxicity, and furthermore, FADS2 inhibitor SC-26196 also reduces ML239 cytotoxicity in cancer cell lines (CCLs).
DC Chemicals, Website:www.dcchemicals.com
Product Name: ML-239|CAS: 1378872-36-6|Cat No: DC10790|Other Names: CID-49843203,CID 49843203,CID49843203,ML-239,ML 239,ML239,1378872-36-6
ML-239 is an inhibitor of cancer stem cells, displaying greater than 23-fold selective inhibition of a breast cancer stem cell-like cell line (EC50 = 1.18 µM) over an isogenic control cell line (EC50 = 27.6 µM).
ML239 (Compound 7j) is a potent and selective inhibitor of breast cancer stem cells, with an IC50 of 1.16 μM, with ∼24-fold selectivity against the control cell line. ML239 inhibits breast cancer stem-like cells, most likely through activation of fatty acid desaturase 2 (FADS2). ML239 is cytotoxic to NCIH661 cells, and FADS2 knockdown reduces ML239 cytotoxicity, and furthermore, FADS2 inhibitor SC-26196 also reduces ML239 cytotoxicity in cancer cell lines (CCLs).
AZD7545|AZD-7545|cas 1816294-67-3
AZD7545|AZD-7545|cas 1816294-67-3
DC Chemicals, Website:www.dcchemicals.com
Product Name: AZD7545|CAS: 1816294-67-3|Cat No: DC10789|Other Names: AZD7545，AZD-7545，AZD 7545
AZD7545 is a novel, selective small-molecule inhibitor of PDHK2 (PDH kinase2) with an IC50 of 36.8 nM and 6.4 nM for PDHK1 and PDHK2 respectively.
AZD7545 is a novel, selective small-molecule inhibitor of PDHK2 (PDH kinase2) with an IC50 of 36.8 nM and 6.4 nM for PDHK1 and PDHK2 respectively. IC50 Value: 36.8 nM (PDHK1); 6.4 nM (PDHK2) [1] Target: PDHK1/2 in vitro: The IC50 values for inhibition of PDHK2 and PDHK1 by AZD7545 were 6.4 ± 2.2 nM (n = 6) and 36.8 ± 18 nM (n = 3) respectively. Other compounds in this series inhibited both PDHK1 and PDHK2 and a consistent trend of reduced potency (5-15-fold) towards PDHK1, as compared with PDHK2, was observed. In contrast, AZD7545 and related compounds failed to inhibit PDHK4 and paradoxically, at higher concentrations (>10 nM), AZD7545 stimulated PDHK4 activity [1]. In the presence of PDHK2, AZD7545 increased PDH activity with an EC(50) value of 5.2 nM. In rat hepatocytes, the rate of pyruvate oxidation was stimulated 2-fold (EC(50) 105 nM) [2]. in vivo: A single dose of AZD7545 to Wistar rats increased the proportion of liver PDH in its active, dephosphorylated form in a dose-related manner from 24.7 to 70.3% at 30 mg/kg; and in skeletal muscle from 21.1 to 53.3%. A single dose of 10 mg/kg also significantly elevated muscle PDH activity in obese Zucker (fa/fa) rats. Obese, insulin-resistant, Zucker rats show elevated postprandial glucose levels compared with their lean counterparts (8.7 versus 6.1 mM at 12 weeks old). AZD7545 (10 mg/kg) twice daily for 7 days markedly improved the 24-h glucose profile, by eliminating the postprandial elevation in blood glucose [2]. An interesting observation is that administration of maximally effective doses of AZD7545 and related compounds to rats results in the near-complete activation of PDH activity in liver, where PDHK2 is the major isoenzyme, while only partial activation of PDH activity is achieved in skeletal muscle and heart, tissues which express high levels of PDHK4. For example, following administration of a maximally effective dose of compound K (30 mg/kg) the percentage of PDH present in the active (dephosphorylated) state in liver is elevated from 35.3 ± 4.0% to 90.2 ± 2.2% while in skeletal muscle and heart PDH activity plateaus at 64.3 ± 2.3% and 61.8 ± 4.3% respectively. Further evidence for a link between in vitro isoenzyme selectivity and in vivo activity comes from the observation that in fasted rats the ability of AZD7545 to elevate PDH activity in liver is intact, while the activation of skeletal muscle PDH activity in response to the compound is severely blunted.
DC Chemicals, Website:www.dcchemicals.com
Product Name: AZD7545|CAS: 1816294-67-3|Cat No: DC10789|Other Names: AZD7545，AZD-7545，AZD 7545
AZD7545 is a novel, selective small-molecule inhibitor of PDHK2 (PDH kinase2) with an IC50 of 36.8 nM and 6.4 nM for PDHK1 and PDHK2 respectively.
AZD7545 is a novel, selective small-molecule inhibitor of PDHK2 (PDH kinase2) with an IC50 of 36.8 nM and 6.4 nM for PDHK1 and PDHK2 respectively. IC50 Value: 36.8 nM (PDHK1); 6.4 nM (PDHK2) [1] Target: PDHK1/2 in vitro: The IC50 values for inhibition of PDHK2 and PDHK1 by AZD7545 were 6.4 ± 2.2 nM (n = 6) and 36.8 ± 18 nM (n = 3) respectively. Other compounds in this series inhibited both PDHK1 and PDHK2 and a consistent trend of reduced potency (5-15-fold) towards PDHK1, as compared with PDHK2, was observed. In contrast, AZD7545 and related compounds failed to inhibit PDHK4 and paradoxically, at higher concentrations (>10 nM), AZD7545 stimulated PDHK4 activity [1]. In the presence of PDHK2, AZD7545 increased PDH activity with an EC(50) value of 5.2 nM. In rat hepatocytes, the rate of pyruvate oxidation was stimulated 2-fold (EC(50) 105 nM) [2]. in vivo: A single dose of AZD7545 to Wistar rats increased the proportion of liver PDH in its active, dephosphorylated form in a dose-related manner from 24.7 to 70.3% at 30 mg/kg; and in skeletal muscle from 21.1 to 53.3%. A single dose of 10 mg/kg also significantly elevated muscle PDH activity in obese Zucker (fa/fa) rats. Obese, insulin-resistant, Zucker rats show elevated postprandial glucose levels compared with their lean counterparts (8.7 versus 6.1 mM at 12 weeks old). AZD7545 (10 mg/kg) twice daily for 7 days markedly improved the 24-h glucose profile, by eliminating the postprandial elevation in blood glucose [2]. An interesting observation is that administration of maximally effective doses of AZD7545 and related compounds to rats results in the near-complete activation of PDH activity in liver, where PDHK2 is the major isoenzyme, while only partial activation of PDH activity is achieved in skeletal muscle and heart, tissues which express high levels of PDHK4. For example, following administration of a maximally effective dose of compound K (30 mg/kg) the percentage of PDH present in the active (dephosphorylated) state in liver is elevated from 35.3 ± 4.0% to 90.2 ± 2.2% while in skeletal muscle and heart PDH activity plateaus at 64.3 ± 2.3% and 61.8 ± 4.3% respectively. Further evidence for a link between in vitro isoenzyme selectivity and in vivo activity comes from the observation that in fasted rats the ability of AZD7545 to elevate PDH activity in liver is intact, while the activation of skeletal muscle PDH activity in response to the compound is severely blunted.
SR-4370|SR4370|HDAC inhibitor|CAS 1816294-67-3
SR-4370|SR4370|HDAC inhibitor|CAS 1816294-67-3
DC Chemicals, Website:www.dcchemicals.com
Product Name: SR-4370|CAS: 1816294-67-3 |Cat No: DC10788|Other Names: SR-4370; SR 4370; SR4370
SR-4370 is an HDAC inhibitor. SR-4370 exhibited IC50 values of 0.5 μM, 0.1 μM and 0.06 μM towards HDAC1, HDAC2 and HDAC3, resp.
DC Chemicals, Website:www.dcchemicals.com
Product Name: SR-4370|CAS: 1816294-67-3 |Cat No: DC10788|Other Names: SR-4370; SR 4370; SR4370
SR-4370 is an HDAC inhibitor. SR-4370 exhibited IC50 values of 0.5 μM, 0.1 μM and 0.06 μM towards HDAC1, HDAC2 and HDAC3, resp.
GSK2982772|GSK-2982772|RIP1 inhibitor
GSK2982772|GSK-2982772|RIP1 inhibitor
DC Chemicals, Website:www.dcchemicals.com
Product Name: GSK2982772|CAS: 1622848-92-3|Cat No: DC10787|Other Names: GSK 2982772，GSK-2982772，GSK2982772，1622848-92-3
GSK2982772 is a potent and ATP competitive RIP1 inhibitor with an IC50 of 16 nM.
DC Chemicals, Website:www.dcchemicals.com
Product Name: GSK2982772|CAS: 1622848-92-3|Cat No: DC10787|Other Names: GSK 2982772，GSK-2982772，GSK2982772，1622848-92-3
GSK2982772 is a potent and ATP competitive RIP1 inhibitor with an IC50 of 16 nM.
PLX51107|PLX-51107|BRD4 inhibitor
PLX51107|PLX-51107|BRD4 inhibitor
DC Chemicals, Website:www.dcchemicals.com
Product Name: PLX51107|CAS: 1627929-55-8|Cat No: DC10786|Other Names: PLX51107，PLX 51107，PLX-51107
PLX51107 is a novel BET inhibitor with a unique binding mode in the acetylated lysine binding pocket of BRD4 that differentiates it from other compounds under investigation.
DC Chemicals, Website:www.dcchemicals.com
Product Name: PLX51107|CAS: 1627929-55-8|Cat No: DC10786|Other Names: PLX51107，PLX 51107，PLX-51107
PLX51107 is a novel BET inhibitor with a unique binding mode in the acetylated lysine binding pocket of BRD4 that differentiates it from other compounds under investigation.
MK-7246|MK7246|cas 1218918-62-7
MK-7246|MK7246|cas 1218918-62-7
DC Chemicals, Website:www.dcchemicals.com
Product Name: MK-7246|CAS: 1218918-62-7|Cat No: DC10785|Other Names: MK7246,MK 7246,MK-7246
MK-7246 is a potent and selective CRTH2 antagonist with a Ki of 2.5±0.5 nM.
The affinity and selectivity of MK-7246 for human CRTH2 and recombinant human prostanoid receptors is determined by equilibrium competition analysis using the relevant radioligands and cell membranes expressing the various receptors. MK-7246 competes for [3H]PGD2 specific binding to cell membranes expressing recombinant human CRTH2 with high-affinity (Ki, 2.5 nM). MK-7246 displays a relatively high selectivity for CRTH2 with an affinity 149-fold lower for the DP receptor (Ki, 373±96 nM) and ≥1500-fold lower for the other prostanoid receptors (Ki, 7668±2169 nM for EP2, 3804±1290 nM for TP). MK-7246 is also tested in a panel of 157 enzyme and receptor assays at concentrations up to 100 μM and small but significant activity is detected only on phosphodiesterase 1 (PDE1, IC50=33.2 μM) and MAPK3 (ERK1, IC50=49.4 μM).Whether the inhibition of a clinically-relevant mechanism of allergic lung inflammation such as CRTH2 will lead to a suppression of inflammatory responses is investigated in A. alternata challenged Brown Norway rats (n=8 per group). Mast cell derived production of Prostaglandin D2 (PGD2) is believed to be a prime mediator of allergic inflammation. Since CRTH2 plays an important role in the early aspects of the allergic inflammation cascade, the effect of the CRTH2 antagonist is examined on A. alternate elicited pulmonary inflammatory responses. CRTH2 inhibitor MK-7246 is orally administered 1 h before and 23 h post-intratracheal instillation of the A. alternata. MK-7246 produces a dose dependent decrease in the number of eosinophils with a maximal inhibition of 74±5% in the 100 mg/kg group (P<0.05), IL-5 (80±12%) and IL-13 (76±14%) cytokines levels (P<0.05).
DC Chemicals, Website:www.dcchemicals.com
Product Name: MK-7246|CAS: 1218918-62-7|Cat No: DC10785|Other Names: MK7246,MK 7246,MK-7246
MK-7246 is a potent and selective CRTH2 antagonist with a Ki of 2.5±0.5 nM.
The affinity and selectivity of MK-7246 for human CRTH2 and recombinant human prostanoid receptors is determined by equilibrium competition analysis using the relevant radioligands and cell membranes expressing the various receptors. MK-7246 competes for [3H]PGD2 specific binding to cell membranes expressing recombinant human CRTH2 with high-affinity (Ki, 2.5 nM). MK-7246 displays a relatively high selectivity for CRTH2 with an affinity 149-fold lower for the DP receptor (Ki, 373±96 nM) and ≥1500-fold lower for the other prostanoid receptors (Ki, 7668±2169 nM for EP2, 3804±1290 nM for TP). MK-7246 is also tested in a panel of 157 enzyme and receptor assays at concentrations up to 100 μM and small but significant activity is detected only on phosphodiesterase 1 (PDE1, IC50=33.2 μM) and MAPK3 (ERK1, IC50=49.4 μM).Whether the inhibition of a clinically-relevant mechanism of allergic lung inflammation such as CRTH2 will lead to a suppression of inflammatory responses is investigated in A. alternata challenged Brown Norway rats (n=8 per group). Mast cell derived production of Prostaglandin D2 (PGD2) is believed to be a prime mediator of allergic inflammation. Since CRTH2 plays an important role in the early aspects of the allergic inflammation cascade, the effect of the CRTH2 antagonist is examined on A. alternate elicited pulmonary inflammatory responses. CRTH2 inhibitor MK-7246 is orally administered 1 h before and 23 h post-intratracheal instillation of the A. alternata. MK-7246 produces a dose dependent decrease in the number of eosinophils with a maximal inhibition of 74±5% in the 100 mg/kg group (P<0.05), IL-5 (80±12%) and IL-13 (76±14%) cytokines levels (P<0.05).
E7820|E-7820|cas 289483-69-8
E7820|E-7820|cas 289483-69-8
DC Chemicals, Website:www.dcchemicals.com
Product Name: E7820|CAS: 289483-69-8|Cat No: DC10784|Other Names: ER68203-00，E7820,E-7820,E 7820,289483-69-8
E7820 is an angiogenesis inhibitor by suppressing integrin a2, a cell adhesion molecule expressed on endothelial cells.
E7820 treatment inhibits proliferation of HUVEC induced by either bFGF and VEGF in serum-free medium with IC50 values of 0.10 and 0.081 μg/mL, respectively. E7820 also inhibits both bFGF- and VEGF-driven tube formation of HUVEC in this assay. The IC50 values are 0.20 and 0.24 μg/mL, respectively.E7820 (50 mg/kg) with erlotinib has a significantly synergistic antitumor effect in three xenograft models without severe body weight loss. E7820 (50 mg/kg) and erlotinib decrease MVD and enhance apoptosis in tumor-associated endothelial cells, inhibit tumor cell proliferation and enhanced apoptosis, and enhance inhibition of cell proliferation and apoptosis through activation of both intrinsic and extrinsic apoptosis pathways in human NSCLC xenograft models. E7820 shows anti-tumor activity at doses of 50, 100, and 200 mg/kg in the tumor growth and α2-integrin expression experiments. E7820 (50, 100, and 200 mg/kg) inhibits tumor growth in a dose-dependent manner in all s.c. xenograft models. E7820 completely inhibits s.c. tumor growth of LoVo tumor cells and also regresses the tumor mass of KP-1 tumor cells at the dosages of both 100 and 200 mg/kg.
DC Chemicals, Website:www.dcchemicals.com
Product Name: E7820|CAS: 289483-69-8|Cat No: DC10784|Other Names: ER68203-00，E7820,E-7820,E 7820,289483-69-8
E7820 is an angiogenesis inhibitor by suppressing integrin a2, a cell adhesion molecule expressed on endothelial cells.
E7820 treatment inhibits proliferation of HUVEC induced by either bFGF and VEGF in serum-free medium with IC50 values of 0.10 and 0.081 μg/mL, respectively. E7820 also inhibits both bFGF- and VEGF-driven tube formation of HUVEC in this assay. The IC50 values are 0.20 and 0.24 μg/mL, respectively.E7820 (50 mg/kg) with erlotinib has a significantly synergistic antitumor effect in three xenograft models without severe body weight loss. E7820 (50 mg/kg) and erlotinib decrease MVD and enhance apoptosis in tumor-associated endothelial cells, inhibit tumor cell proliferation and enhanced apoptosis, and enhance inhibition of cell proliferation and apoptosis through activation of both intrinsic and extrinsic apoptosis pathways in human NSCLC xenograft models. E7820 shows anti-tumor activity at doses of 50, 100, and 200 mg/kg in the tumor growth and α2-integrin expression experiments. E7820 (50, 100, and 200 mg/kg) inhibits tumor growth in a dose-dependent manner in all s.c. xenograft models. E7820 completely inhibits s.c. tumor growth of LoVo tumor cells and also regresses the tumor mass of KP-1 tumor cells at the dosages of both 100 and 200 mg/kg.
订阅：
博文 (Atom)