2016年10月8日星期六

Valbenazine(NBI-98854)|VMAT2 inhibitor

Valbenazine(NBI-98854)|VMAT2 inhibitor


Valbenazine(NBI-98854) is a potent and selective VMAT2 inhibitor..

Product Name: Valbenazine(NBI-98854)|Cat No. DC9816|CAS: 1025504-45-3|Other names:NBI-98854; NBI 98854; NBI98854; Valbenazine|MW: 418.28|Molecule Formular: C24H38N2O4 |Purity>98%

Valbenazine, aslo known as NBI-98854, is a potent and selective VMAT2 inhibitor. NBI-98854 is effective in regulating the levels of dopamine release during nerve communication, while at the same time having minimal impact on the other monoamines. NBI-98854 is promising agent for the treatment of tardive dyskinesia.NBI-98854 significantly improved tardive dyskinesia and was well tolerated in patients. These results support the phase 3 clinical trials of NBI-98854 now underway.

Pimodivir(VX-787,VX787)|antiviral agent/inhibitor

Pimodivir(VX-787,VX787)|antiviral agent/inhibitor

Pimodivir(VX-787) is a novel inhibitor of influenza virus replication that blocks the PB2 cap-snatching activity of the influenza viral polymerase complex.

Product Name: Pimodivir(VX-787)|Cat No. DC9815|CAS: 1629869-44-8|Other names:VX-787; VX 787; VX787; JNJ-872; JNJ 872; JNJ872; VRT-0928787; VRT 0928787; VRT0928787;pimodivir|MW: 399.15|Molecule Formular: C20H19F2N5O2|Purity>98%

rus replication that blocks the PB2 cap-snatching activity of the influenza viral polymerase complex. Viral genetics and X-ray crystallography studies provide support for the idea that VX-787 occupies the 7-methyl GTP (m(7)GTP) cap-binding site of PB2. VX-787 binds the cap-binding domain of the PB2 subunit with a KD (dissociation constant) of 24 nM as determined by isothermal titration calorimetry (ITC). The cell-based EC50 (the concentration of compound that ensures 50% cell viability of an uninfected control) for VX-787 is 1.6 nM in a cytopathic effect (CPE) assay, with a similar EC50 in a viral RNA replication assay. VX-787 is active against a diverse panel of influenza A virus strains, including H1N1pdm09 and H5N1 strains, as well as strains with reduced susceptibility to neuraminidase inhibitors (NAIs). VX-787 was highly efficacious in both prophylaxis and treatment models of mouse influenza and was superior to the neuraminidase inhibitor, oseltamivir, including in delayed-start-to-treat experiments, with 100% survival at up to 96 h postinfection and partial survival in groups where the initiation of therapy was delayed up to 120 h postinfection. At different doses, VX-787 showed a 1-log to >5-log reduction in viral load (relative to vehicle controls) in mouse lungs. Overall, these favorable findings validate the PB2 subunit of the viral polymerase as a drug target for influenza therapy and support the continued development of VX-787 as a novel antiviral agent for the treatment of influenza infection.

PLX7904(PB04)|paradox-breaker RAF inhibitor

PLX7904(PB04)|paradox-breaker RAF inhibitor

PLX7904(PB04) is a potent and selective paradox-breaker RAF inhibitor.

Product Name: PLX7904(PB04)|Cat No. DC9814|CAS: 1393465-84-3|Other names:PLX-7904,PLX 7907,PB04; PB-04; PB 04; paradox-breaker-04|MW: 512.14|Molecule Formular: C24H22F2N6O3S|Purity>98%

PLX7904, also known as PB04, is a potent and selective paradox-breaker RAF inhibitor. PB04 is able to efficiently inhibit activation of ERK1/2 in mutant BRAF melanoma cells but does not hyperactivate ERK1/2 in mutant RAS-expressing cells. Importantly, PB04 inhibited ERK1/2 phosphorylation in mutant BRAF melanoma cells with acquired resistance to vemurafenib/PLX4720 that is mediated by a secondary mutation in NRAS. Consistent with ERK1/2 reactivation driving the re-acquisition of malignant properties, PB04 promoted apoptosis and inhibited entry into S phase and anchorage-independent growth in mutant N-RAS-mediated vemurafenib-resistant cells.


Valspodar(PSC833)|P-glycoprotein (P-gp) inhibitor

Valspodar(PSC833)|P-glycoprotein (P-gp) inhibitor

Valspodar(PSC833) is a P-glycoprotein (P-gp) inhibitor widely used in preclinical and clinical studies for overcoming multidrug resistance (MDR).

Product Name: Valspodar(PSC833)|Cat No. DC9813|CAS: 121584-18-7|Other names:PSC 833; PSC-833; PSC833|MW: 1214.62|Molecule Formular: C63H111N11O12|Purity>98%

Valspodar(PSC833) is a P-glycoprotein (P-gp) inhibitor widely used in preclinical and clinical studies for overcoming multidrug resistance (MDR). In rat, Valspodar showed properties of low hepatic extraction and wide distribution, similar to that of its structural analogue cyclosporine A. Administration of Valspodar to animals before mitoxantrone treatment increased the accumulation of mitoxantrone in the MDR tumors to 94% of that in the wild-type tumors. These studies have added direct in vitro and in vivo visual information on how P-gp processes anticancer compounds and how P-gp inhibitors modulate MDR in resistant cancer cells.

Wnt Inhibitor IWP-4|Differentiation Inducer

Wnt Inhibitor IWP-4|Differentiation Inducer

Wnt Inhibitor IWP-4 is a potent inhibitor of Wnt/β-catenin signaling (IC50 = 25 nM).

Product Name: IWP-4|Cat No. DC9812|CAS: 686772-17-8|Other names:IWP4,IWP 4|MW: 496.6|Molecule Formular: C23H20N4O3S3|Purity>98%

Wnt Inhibitor IWP-4 was identified in a high throughput screen for antagonists of the Wnt / β-catenin pathway. Wnt Inhibitor IWP-4 prevents palmitylation of Wnt proteins by Porcupine (Porcn), a membrane-bound O-acyltransferase, there by blocking Wnt secretion and activity. It also blocks phosphorylation of the Lrp6 receptor and accumulation of both Dvl2 and β-catenin. IWP-4 has been shown to block Wnt-dependent phosphorylation of the low-density lipoprotein receptor-related protein 6 receptor and the scaffold protein Dishevelled, preventing the accumulation of β-catenin. IWP-4 has been used to induce cardiomyocyte differentiation from human pluripotent stem cells.

PT2399|PT-2399|HIF2α Antagonist

PT2399|PT-2399|HIF2α Antagonist

PT2399(PT=2399) is a novel HIF2α Antagonist.

Product Name: PT2399|Cat No. DC9811|CAS: N/A|Other names:PT2399,PT 2399,PT-2399|MW: 419.03|Molecule Formular: C17H10F5NO4S|Purity>98%

PT2399(PT=2399) is a novel HIF2α Antagonist. PT2399 directly inhibits HIF2α causes tumor regression in preclinical models of primary and metastatic pVHL-

ND-646 |ND646|ACC inhibitor

ND-646 |ND646|ACC inhibitor

ND-646(ND646) is a small-molecule allosteric inhibitor of acetyl-CoA carboxylase (ACC).

Product Name: ND-646|Cat No. DC9810|CAS: N/A|Other names:ND646,ND 646|MW: 568.2|Molecule Formular: C17H10F5NO4S|Purity>98%

ND-646 is an allosteric inhibitor of the ACC enzymes ACC1 and ACC2 that prevents ACC subunit dimerization—to suppress fatty acid synthesis in vitro and in vivo.

APS-3-77|KSR/RAS signaling modulator

APS-3-77|KSR/RAS signaling modulator

APS-3-77 is a novel modulator of KSR-dependent MAPK signalling,KSR2,IC50>10 uM

Product Name: APS-3-77|Cat No. DC9809|CAS: N/A|Other names:APS 3 77,APS377,APS-377|MW: 401.17|Molecule Formular: C24H23N3O3|Purity>98%

APS-3-77 is a novel modulator of KSR-dependent MAPK signalling,KSR2,IC50>10 Um,antagonizing RAF heterodimerization as well as the conformational changes required for phosphorylation and activation of KSR-bound MEK (mitogen-activated protein kinase)


APS-2-79|KSR/RAS signaling modulator

APS-2-79|KSR/RAS signaling modulator

APS-2-79 is a novel modulator of KSR-dependent MAPK signalling,KSR2,IC50=120 nM

Product Name: APS-2-79|Cat No. DC9808|CAS: N/A|Other names:APS 2 79,APS279,APS-279|MW: 387.16|Molecule Formular: C23H21N3O3|Purity>98%

APS-2-79 is a novel modulator of KSR-dependent MAPK signalling, antagonizing RAF heterodimerization as well as the conformational changes required for phosphorylation and activation of KSR-bound MEK (mitogen-activated protein kinase)

S-2238,S2238(Thrombin Chromogenic Substrate)

S-2238,S2238(Thrombin Chromogenic Substrate)

S-2238 is specific to thrombin, is a short peptide covalently bound to pNA (4-nitroaniline).

Product Name: S-2238(Thrombin Substrate)|Cat No. DC9807|CAS: 115388-96-0|Other names:S 2238,S-2238|MW: 625.6|Molecule Formular: H-D-Phe-Pip-Arg-pNA·

S-2238, which is specific to thrombin, is a short peptide covalently bound to pNA (4-nitroaniline). When attacked by thrombin, it gives up a free pNA which could


S-2765,S2765 (Fxa Chromogenic substrate)

S-2765,S2765 (Fxa Chromogenic substrate)

S-2765 is specific to activated factor X (FXa),short peptide covalently bound to pNA (4-nitroaniline).

Product Name: S-2765(FXa substrate)|Cat No. DC9806|CAS: 113711-77-6|Other names:S2765 ,S 2765 |MW: 714.6|Molecule Formular: Z-D-Arg-Gly-Arg-pNA·2HCl|Purity>98%

S-2765, which is specific to activated factor X (FXa), is a short peptide covalently bound to pNA (4-nitroaniline). When attacked by FXa, it releases a free pNA which could be detected by a spectrophotometer at 405 nm.S-2765 is mainly used in anti-FXa activity assay of heparin. S-2765 can be used in many applications, such as:
1:Anti-factor Xa activity to anti-factor IIa activity ratios of heparin and LMWHs.
2: Anti-factor Xa activities of heparin and LMWHs.
3: Activities of antithrombin and coagulation factors.
4: Anti-factor Xa activities of heparin and LMWHs in human plasma.
5: Production of kits for automated blood analyzers.
6: Evaluation of potential anticoagulants from chemical synthesis, bacterial fermentation and animal tissues.

Preladenant(SCH420814)|adenosine A2A receptor antagonist

Preladenant(SCH420814)|adenosine A2A receptor antagonist

Preladenant(SCH 420814) is a potent and selective antagonist at the adenosine A2A receptor.

Product Name: Preladenant(SCH420814)|Cat No. DC9805|CAS: 377727-87-2|Other names:SCH-420814; SCH 420814; SCH420814|MW: 503.56|Molecule Formular: C25H29N9O3|Purity>98%

The adenosine A(2A) receptor has been implicated in the underlying biology of various neurological and psychiatric disorders, including Parkinson's disease (PD)

Masitinib|PDGFR inhibitor

Masitinib|PDGFR inhibitor

Masitinib(AB-1010) is a novel inhibitor for Kit and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, weak inhibition to ABL and c-Fms.

Product Name: Masitinib|Cat No. DC9804|CAS: 790299-79-5|Other names:AB1010;  Masivet;  AB-1010;  AB 1010|MW: 498.64|Molecule Formular: C28H30N6OS|Purity>98%

Masitinib(AB-1010) is a novel inhibitor for Kit and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, weak inhibition to ABL and c-Fms.
in vitro: In Ba/F3 cells expressing human wild-type Kit, Masitinib inhibits SCF (stem cell factor)-induced cell proliferation with an IC50 of 150 nM, while the IC50 for inhibition of IL-3-stimulated proliferation is at approximately >10 μM. In Ba/F3 cells expressing PDGFRα, Masitinib inhibits PDGF-BB-stimulated proliferation and PDGFRα tyrosine phosphorylation with IC50 of 300 nM. Masitinib also causes inhibition of SCF-stimulated tyrosine phosphorylation of human Kit in mastocytoma cell-lines and BMMC. Masitinib inhibits Kit gain-of-function mutants, including V559D mutant and Δ27 mouse mutant with IC50 of 3 and 5 nM in Ba/F3 cells. Masitinib inhibits the cell proliferation of mastocytoma cell lines including HMC-1α155 and FMA3 with IC50 of 10 and 30 nM, respectively [1]. Masitinib inhibits cell growth and PDGFR phosphorylation in two novel ISS cell lines, which suggest that Masitinib displays activity against both primary and metastatic ISS cell line and may aid in the clinical management of ISS.
in vivo: Masitinib inhibits tumour growth and increases the median survival time in Δ27-expressing Ba/F3 tumor models at 30 mg/kg, without cardiotoxicity or genotoxicity [1]. Masitinib (12.5 mg/kg/d PO) increases overall TTP (time-to-tumor progression) compared with placebo in dogs.

CMP8|CMP-8|ligand of mutant ERLBD

CMP8|CMP-8|ligand of mutant ERLBD

CMP8 is a high-affinity ligand that binds only to mutant ERLBD.

Product Name: CMP8|Cat No. DC9803|CAS: N/A|Other names:CMP 8,CMP-8|MW: 527.22|Molecule Formular: C33H34ClNO3|Purity>98%

CMP8 is a high-affinity ligand that binds only to mutant ERLBD.

23-hydroxy butulinic acid (23-HBA)

23-hydroxy butulinic acid (23-HBA)

23-hydroxy butulinic acid (23-HBA) is a potent angiogenesis inhibitor.

Product Name: 23-hydroxy butulinic acid (23-HBA)|Cat No. DC9802|CAS: 85999-40-2|Other names:|MW: 472.71|Molecule Formular: C30H48O4|Purity>98%

23-HBA can inhibit angiogenesis in vitro.The proliferation of HMECs was inhibited significantly by 23-HBA with IC(50) being 40.44 mg/L. 23-HBA inhibited endothelial cell migration and tubule formation in a dose-dependent manner. The expression of CD31 in HMECs was reduced after treatment with 10 mg/L 23-HBA.


GSK3183475|GSK-3183475|DC Chemicals

GSK3183475|GSK-3183475|DC Chemicals

Product Name: GSK3183475|Cat No. DC9801|CAS: N/A|Other names:GSK-3183475,GSK 3183475|MW: 379.2|Molecule Formular: C21H25N5O2|Purity>98%




GSK-3206906|GSK3206906|DC Chemicals

GSK-3206906|GSK3206906|DC Chemicals

GSK-3206906|GSK3206906|DC Chemicals

Product Name: GSK3206906|Cat No. DC9800|CAS: N/A|Other names:GSK-3206906,GSK 3206906|MW: 480.12|Molecule Formular: C22H17F5N4O3|Purity>98%


CNDAC|active component of sapacitabine

CNDAC|active component of sapacitabine

CNDAC is the active component of sapacitabine.

Product Name: CNDAC|Cat No. DC9799|CAS: 135598-68-4|Other names:|MW: 250.11|Molecule Formular: C11H14N4O3|Purity>98%

CNDAC is the active component of sapacitabine. Sapacitabine is an oral nucleoside analog prodrug that acts through a dual mechanism. The compound interferes with DNA synthesis by causing single-strand DNA breaks and induces arrest of the cell division cycle at G2 phase.Both sapacitabine and its major metabolite, CNDAC, have demonstrated potent anti-tumor activity in both blood and solid tumors in preclinical studies. In a liver metastatic mouse model, sapacitabine was shown to be superior to gemcitabine or 5-FU, two widely used nucleoside analogs, in delaying the onset and growth of liver metastasis.

Leteprinim (Neotrofin, AIT-082)

Leteprinim (Neotrofin, AIT-082)

Leteprinim (Neotrofin, AIT-082) is a hypoxanthine derivative drug with neuroprotective and nootropic effects.

Product Name: Leteprinim|Cat No. DC9798|CAS: 138117-50-7|Other names:Neotrofin, AIT-082|MW: 327.3|Molecule Formular: C15H13N5O4|Purity>98%

Leteprinim (Neotrofin, AIT-082) is a hypoxanthine derivative drug with neuroprotective and nootropic effects.It stimulates release of nerve growth factors and enhances survival of neurons in the brain,and is under development as a potential treatment for neurodegenerative disorders such as Alzheimer's disease, Parkinson's disease and stroke.

CLR1501|CLR-1501|tumor-targeting imaging compound

CLR1501|CLR-1501|tumor-targeting imaging compound

CLR1501 is a synthetic analogs of the tumor-targeting agent alkylphosphocholine (APC), which is specifically attracted to cancer cells.

Product Name: CLR1501|Cat No. DC9797|CAS: N/A|Other names:|MW: 701.43|Molecule Formular: C38H59BF2N3O4P|Purity>98%

CLR1501 is a synthetic analogs of the tumor-targeting agent alkylphosphocholine (APC), which is specifically attracted to cancer cells. CLR1501 is molecularly

Nicainoprolhe|cas 76252-06-7

Nicainoprolhe|cas 76252-06-7

Nicainoprolhe is an antiarrhythmic agent,a fast-sodiumchannel blocking drug (class Ib), also protected isolated rat hearts against reperfusion arrhythmias.

Product Name: Nicainoprolhe|Cat No. DC9796|CAS: 76252-06-7|Other names:|MW: 369.45|Molecule Formular: C21H27N3O3|Purity>98%


HA15|HA-15|CAS 1609402-14-3

HA15|HA-15|CAS 1609402-14-3

HA15 displayed anti-cancerous activity on all melanoma cells tested, including cells isolated from patients and cells that developed resistance to BRAF inhibitors.

Product Name: HA-15|Cat No. DC9795|CAS: 1609402-14-3 |Other names:HA15,HA 15|MW: 466.11|Molecule Formular: C23H22N4O3S2|Purity>98%

HA15 displayed anti-cancerous activity on all melanoma cells tested, including cells isolated from patients and cells that developed resistance to BRAF inhibitors. HA15 also exhibited strong efficacy in xenograft mouse models with melanoma cells either sensitive or resistant to BRAF inhibitors. Transcriptomic, proteomic, and biochemical studies identified the chaperone BiP/GRP78/HSPA5 as the specific target of HA15 and demonstrated that the interaction increases ER stress, leading to melanoma cell death by concomitant induction of autophagic and apoptotic mechanisms.

SU10994|SU-10994|VEGFR inhibitor

SU10994|SU-10994|VEGFR inhibitor

SU-10994 is a novel VEGFR inhibitor.

Product Name: SU-10994|Cat No. DC9794|CAS: N/A|Other names:SU10994,SU 10994|MW: 296.12|Molecule Formular: C17H16N2O3|Purity>98%

AMG-232 is a novel inhibitor of p53-MDM2 with IC50 value of 9.2 nM.
Tumor protein p53 (p53) is a very unstable protein with a half-life ranging from 5 to 30 min and participates in a variety of anticancer processes, such as inducing cell apoptosis and inhibiting angiogenesis. Mouse double minute 2 homolog (MDM2), also named as E3 ubiquitin-protein ligase Mdm2, involves in mediating p53 tumor suppressor. It has been conclusively demonstrated p53 is under-expressed in tumor cells.
AMG-232 is a potent p53-MDM2 interaction inhibitor and is regarded as a promising drug in clinic. When tested with SJSA-1 tumor cell line, AMG-232 treatment resulted in cell-cycle arrest and inhibition of tumor cell proliferation via binding to MDM2 protein and robustly inducing p53 activity. It was shown that p53-MDM2 bond rang from a Kd of 60 to 700 nM Depending on the length of p53 peptide.
In mouse model with SJSA-1 tumor cells subcutaneous xenograft, co-administration of AMG-232 and chemotherapies induced DNA damage and p53 activity which resulted in significantly superior antitumor efficacy and regression through arresting cell growth and inducting apoptosis.

AMG232|AMG-232|MDM2−p53 inhibitor

AMG232|AMG-232|MDM2−p53 inhibitor

AMG232 is a potent, selective and orally bioavailable inhibitor of MDM2−p53 interaction with IC50 value of 9.1 nM in EdU cells .

Product Name: AMG232|Cat No. DC9793|CAS: 1352066-68-2|Other names:AMG-232,AMG 232|MW: 568.55|Molecule Formular: C28H35Cl2NO5S|Purity>98%

AMG-232 is a novel inhibitor of p53-MDM2 with IC50 value of 9.2 nM.

SAR20106|SAR020106|CHK1 inhibitor

SAR20106|SAR020106|CHK1 inhibitor

SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC(50) of 13.3 nmol/L on the isolated human enzyme.

Product Name: SAR020106|Cat No. DC9792|CAS: 1184843-57-9|Other names:SAR020106; SAR020106; SAR 020106; SAR20106; SAR20106; SAR 20106|MW: 382.13|Molecule Formular: C19H19ClN6O |Purity>98%

SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC(50) of 13.3 nmol/L on the isolated human enzyme. This compound abrogates an etoposide-induced G(2) arrest with an IC(50) of 55 nmol/L in HT29 cells, and significantly enhances the cell killing of gemcitabine and SN38 by 3.0- to 29-fold in several colon tumor lines in vitro and in a p53-dependent fashion. Biomarker studies have shown that SAR-020106 inhibits cytotoxic drug-induced autophosphorylation of CHK1 at S296 and blocks the phosphorylation of CDK1 at Y15 in a dose-dependent fashion both in vitro and in vivo. SAR-020106 represents a novel class of CHK1 inhibitors that can enhance antitumor activity with selected anticancer drugs in vivo and may therefore have clinical utility.


BLU-554|BLU554|FGFR4 inhibitor

BLU-554|BLU554|FGFR4 inhibitor

BLU-554 is an isoform selective inhibitor of fibroblast growth factor (FGF) receptor 4 (FGFR4; CD334)

Product Name: BLU-554 (FGFR4 inhibitor)|Cat No. DC9791|CAS: 1707289-21-1|Other names:BLU-554,BLU554,BLU 554|MW: 503.38|Molecule Formular: C24H24Cl2N4O4|Purity>98%

BLU-554 targets the fibroblast growth factor receptor 4 (FGFR4), while sparing other members of the FGFR family and showing little to no inhibition of all other kinases. Aberrant signaling of FGFR4 is a key driver in up to 30 percent of HCC, and BLU-554 has shown significant anti-tumor activity, including complete and sustained tumor regression, in preclinical models of HCC. Initial clinical development will target aberrant FGFR4 activation in HCC and will assess the safety and preliminary efficacy of BLU-554 in treatment-naïve HCC patients and patients that have failed sorafenib, the only approved systemic therapy for HCC.

Nazartinib(EGF816,EGF-816)|EGFR-T790M inhibitor

Nazartinib(EGF816,EGF-816)|EGFR-T790M inhibitor

Nazartinib(EGF816) is a novel covalent inhibitor of mutant-selective EGFR; overcomes T790M-mediated resistance in NSCLC.

Product Name: Nazartinib(EGF816)|Cat No. DC9790|CAS: 1508250-71-2|Other names:EGF-816,EGF 816|MW: 495.02|Molecule Formular: C26H31ClN6O2|Purity>98%

Icaritin(Anhydroicaritin)|IL-6/JAK2/STAT3 inhibitor

Icaritin(Anhydroicaritin)|IL-6/JAK2/STAT3 inhibitor

Icaritin shows potent anti-leukemia activity on chronic myeloid leukemia in vitro and in vivo by regulating MAPK/ERK/JNK and JAK2/STAT3 /AKT signalings.

Product Name: Icaritin(Anhydroicaritin)|Cat No. DC9789|CAS: 118525-40-9|Other names:|MW: 368.38|Molecule Formular: C21H20O6|Purity>98%

Icaritin is an active prenylflavonoid derived from Epimedium genus, a traditional Chinese medicine. Icaritin has a wide range of pharmacological and biological activities, including cardiovascular function improvement, hormone regulation and antitumor activity. Icaritin shows potent anti-leukemia activity on chronic myeloid leukemia in vitro and in vivo by regulating MAPK/ERK/JNK and JAK2/STAT3 /AKT signalings. Icaritin potently inhibited proliferation of K562 cells (IC50 was 8 µM) and primary CML cells (IC50 was 13.4 µM for CML-CP and 18 µM for CML-BC), induced CML cells apoptosis and promoted the erythroid differentiation of K562 cells with time-dependent manner. Furthermore, Icaritin was able to suppress the growth of primary CD34+ leukemia cells (CML) and Imatinib-resistant cells, and to induce apoptosis. In mouse leukemia model, Icaritin could prolong lifespan of NOD-SCID nude mice inoculated with K562 cells as effective as Imatinib without suppression of bone marrow. Icaritin could up-regulate phospho-JNK or phospho-C-Jun and down-regulate phospho-ERK, phospho-P-38, Jak-2, phospho-Stat3 and phospho-Akt expression with dose- or time-dependent manner. Icaritin had no influence both on c-Abl and phospho-c-Abl protein expression and mRNA levels of Bcr/Abl.

KP1019(FFC14A)|KP-1019|ruthenium anticancer agent

KP1019(FFC14A)|KP-1019|ruthenium anticancer agent

KP1019 (FFC14A) is just the second ruthenium-based anticancer agent after NAMI-A which was developed to the stage of clinical trials.

Product Name: KP1019(FFC14A)|Cat No. DC9788|CAS: 124875-20-3|Other names:KP1019; KP 1019; KP1019; FFC14A; indazolium

KP1019, also known as FFC14A, is just the second ruthenium-based anticancer agent after NAMI-A which was developed to the stage of clinical trials. Important steps

NAMI-A|NAMIA|ruthenium anticancer agent

NAMI-A|NAMIA|ruthenium anticancer agent

NAMI-A is a ruthenium anticancer agent and a metastasis inhibitor.

Product Name: NAMI-A|Cat No. DC9787|CAS: 201653-76-1 |Other names:NAMIA,NAMI A|MW: 458.18|Molecule Formular: C8H15Cl4N4ORuS |Purity>98%

NAMI-A is a ruthenium anticancer agent and a metastasis inhibitor. NAMI is an acronym for "New Anti-tumour Metastasis Inhibitor", while the -A suffix indicates

NKP-1339|NKP-1339|ruthenium-based anticancer drug

NKP-1339|NKP-1339|ruthenium-based anticancer drug

NKP-1339 is the first-in-class ruthenium-based anticancer drug in clinical development against solid cancer and has recently been studied successfully in a phase I clinical trial.

Product Name: NKP-1339|Cat No. DC9786|CAS: 197723-00-5|Other names:KP1339,KP 1339,NKP1339,NKP 1339,KP-1339|MW: 502.14|Molecule Formular: C14H12Cl4N4NaRu|Purity>98%

IMR1A|IMR 1A|Notch inhibitor

IMR1A|IMR 1A|Notch inhibitor

IMR-1A is the metabolite of IMR-1. IMR-1 is a novel class of Notch inhibitors targeting the transcriptional activation with IC50 of 6 μmol/L.

Product Name: IMR-1A|Cat No. DC9785|CAS: 331862-41-0|Other names:IMR1A,IMR 1A,IMR-1A|MW: 325.36|Molecule Formular: C13H11NO5S2|Purity>98%

MR-1A is the metabolite of IMR-1. IMR-1 is a novel class of Notch inhibitors targeting the transcriptional activation with IC50 of 6 μmol/L.

Lu AF21934|modulator of mGlu4 receptor

Lu AF21934|modulator of mGlu4 receptor

Lu AF21934 is a brain-penetrating positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu4),reduces the harmaline-induced hyperactivity

Product Name: Lu AF21934|Cat No. DC9784|CAS: 1445605-23-1|Other names:Lu AF-21934,Lu AF 21934,Lu-AF21934,Lu-AF-21934|MW: 314.1|Molecule Formular:

Lu AF21934 is a brain-penetrating positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu4), on the harmaline-induced tremor and other forms

Bay 59-3074|CB1/CB2 receptor partial agonist

Bay 59-3074|CB1/CB2 receptor partial agonist

Bay 59-3074 is a novel CB1/CB2 receptor partial agonist (Ki values are 48.3 and 45.5 nM at human CB1 and CB2 receptors respectively).

Product Name: Bay 59-3074|Cat No. DC9783|CAS: 406205-74-1|Other names:BAY-59-3074; BAY 59-3074; BAY59-3074|MW: 453.35|Molecule Formular: C18H13F6NO4S|Purity>98%

Bay 59-3074 is a novel CB1/CB2 receptor partial agonist (Ki values are 48.3 and 45.5 nM at human CB1 and CB2 receptors respectively). Orally active CB1 agonist in

SR 3029|SR3029|CK1δ/ε inhibitor|1454585-06-8

SR 3029|SR3029|CK1δ/ε inhibitor|1454585-06-8


SR 3029 is a potent and highly specific CK1δ/CK1ε inhibitor with the IC50 of 97 nM.

Product Name: SR-3029|Cat No. DC9782|CAS: 1454585-06-8|Other names:SR3029,SR 3029|MW: 480.45|Molecule Formular: C23H19F3N8O|Purity>98%

SR 3029 is a potent and highly specific CK1δ/CK1ε inhibitor with the IC50 of 97 nM.

SU-4312,SU4312|VEGFR inhibitor

SU-4312,SU4312|VEGFR inhibitor

SU-4312 is a selective and potent vascular endothelial cell growth factor receptor (VEGFR) inhibitor.

Product Name: SU4312|Cat No. DC9781|CAS: 5812-07-7|Other names:SU 4312,SU-4312|MW: 264.3|Molecule Formular: C17H16N2O|Purity>98%

SU 4312 is a selective and potent vascular endothelial cell growth factor receptor (VEGFR) inhibitor. Inhibition of Flk-1 (VEGFR-2) in neonatal rodent models of stroke, has been shown to limit endothelial cell proliferation and promote cell death. SU 4312 is an inhibitor of Flg, Flt-1 and PDGFR-β.

Tenofovir disoproxil|cas 201341-05-1

Tenofovir disoproxil|cas 201341-05-1

Tenofovir is an antiretroviral drug known as nucleotide analogue reverse transcriptase inhibitors (NRTIs), which block reverse transcriptase, a crucial virus enzyme in HIV-1 and HBV.

Product Name: Tenofovir disoproxil|Cat No. DC9780|CAS: 201341-05-1|Other names:|MW: 519.44|Molecule Formular: C19H30N5O10P|Purity>98%

Sildenafil citrate|PDE5 inhibitor

Sildenafil citrate|PDE5 inhibitor

Sildenafil citrate, one of the selective phosphodiesterase-5 (PDE5) inhibitors(IC50= 5.22 nM), is considered the best treatment for erectile dysfunction.

Product Name: Sildenafil citrate|Cat No. DC9779|CAS: 171599-83-0|Other names:|MW: 666.7|Molecule Formular: C28H38N6O11S|Purity>98%

Zoledronic Acid|activator of protein kinase C

Zoledronic Acid|activator of protein kinase C

Zoledronic acid(CGP 42446; ZOL 446) is an activator of protein kinase C with apoptotic effects on multiple myeloma cell lines. It inhibited proliferation of human foetal osteoblastic cell line (hFOB) with an IC50 of 40 uM.

Product Name: Zoledronic Acid|Cat No. DC9778|CAS: 118072-93-8|Other names:CGP 42446; ZOL 446|MW: 272.09|Molecule Formular: C5H10N2O7P2|Purity>98%

Regorafenib monohydrate|VEGFR inhibitor

Regorafenib monohydrate|VEGFR inhibitor

Regorafenib (BAY 73-4506) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.

Product Name: Regorafenib monohydrate(BAY 73-4506)|Cat No. DC9777|CAS: 1019206-88-2|Other names:|MW: 500.83|Molecule Formular: C21H17ClF4N4O4|Purity>98%


Pazopanib Hcl (GW-786034)|VEGFR inhibitor

Pazopanib Hcl (GW-786034)|VEGFR inhibitor

Pazopanib Hcl (GW-786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM, respectively.

Product Name: Pazopanib Hydrochloride|Cat No. DC9776|CAS: 635702-64-6|Other names:GW-786034,GW786034,GW 786034|MW: 473.98|Molecule Formular: C21H24ClN7O2S|Purity>98%


WZ3146|WZ-3146|EGFR(L858R,E746_A750) inhibitor

WZ3146|WZ-3146|EGFR(L858R,E746_A750) inhibitor

WZ3146 is a mutant-selective irreversible inhibitor of EGFR(L858R) and EGFR(E746_A750) with IC50 of 2 nM and 2 nM; does not inhibit ERBB2 phosphorylation (T798I).

Product Name: WZ3146|Cat No. DC9775|CAS: 1214265-56-1|Other names:WZ 3146,WZ-3146|MW: 464.95|Molecule Formular: C24H25ClN6O2|Purity>98%

LEE011 succinate|CDK inhibitor

LEE011 succinate|CDK inhibitor

LEE011 succinate is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity.

Product Name: LEE011 succinate|Cat No. DC9774|CAS: 1374639-75-4|Other names:Ribociclib; LEE 011; LEE-011|MW: 552.63|Molecule Formular: C27H36N8O5|Purity>98%

LEE011 hydrochloride|CDK inhibitor

LEE011 hydrochloride|CDK inhibitor

LEE011 Hcl is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity.

Product Name: LEE011 hydrochloride|Cat No. DC9773|CAS: 1211443-80-9|Other names:Ribociclib; LEE 011; LEE-011|MW: 471.0|Molecule Formular: C23H31ClN8O|Purity>98%

Efinaconazole(KP-103)|antifungal drug

Efinaconazole(KP-103)|antifungal drug

Efinaconazole(KP-103) is a novel triazole antifungal drug currently under development as a topical treatment for onychomycosis.

Product Name: Efinaconazole(KP-103)|Cat No. DC9772|CAS: 164650-44-6|Other names:Jublia, KP 103, KP103|MW: 348.39|Molecule Formular: C18H22F2N4O|Purity>98%

Emixustat|ACU-4429|cas 1141934-97-5

Emixustat|ACU-4429|cas 1141934-97-5

Emixustat hydrochloride strongly inhibits 11-cis-retinol production with IC50 values of 232 ± 3 nM.

Product Name: Emixustat (ACU-4429)|Cat No. DC9771|CAS: 1141934-97-5|Other names:ACU4429,ACU 4429,ACU-4429|MW: 299.84|Molecule Formular: C16H26ClNO2|Purity>98%

Emixustat hydrochloride is a novel visual cycle modulator, in healthy volunteers. Oral Emixustat was safe and well tolerated when administered once daily for 14 days with minimal systemic adverse events reported. Evaluation of emixustat in subjects with geographic atrophy associated with dry age-related macular degeneration.

NCB-0846|NCB0846|TNIK/Wnt inhibitor|Cancer stemcell

NCB-0846|NCB0846|TNIK/Wnt inhibitor|Cancer stemcell

NCB-0846 is a novel,first-in-class,orally TNIK inhibitor with an IC50 value of 21 nM,that have shown strong anti-tumor efficacy against several cancer models.

Product Name: NCB-0846|Cat No. DC9770|CAS: N/A|Other names:NCB0846,NCB 0846|MW: 375.17|Molecule Formular: C21H21N5O2|Purity>98%

NCB-0846 is novel,first-in-class,orally TNIK inhibitor with an IC50 value of 21 nM,that have shown strong anti-tumor efficacy against several cancer models.NCB-0846 suppresses Wnt-driven intestinal tumorigenesis in Apcmin/+ mice and the sphere- and tumour-forming activities of colorectal cancer cells. NCB-0846 inhibits cancer cell growth in vitro and in vivo.NCB-0846 induced faster migration of TCF4 phosphorylated by TNIK within a concentration range of 0.1–0.3 μM  and completely inhibited the phosphorylation of TCF4 at a concentration of 3 μM . Furthermore, NCB-0846 blocked the auto-phosphorylation of TNIK). NCB-0846 inhibited the TCF/LEF transcriptional activity of Wnt3a-treated HEK293  and HCT116 (carrying CTNNB1 mutation) and DLD-1 (carrying APC mutation) colorectal cancer  cells. NCB-0846 reduced the expression of the Wnt target genes AXIN2 and MYC as well as that of TNIK, but the expression of CCND1 was not affected .NCB-0846 also reduced the expression of TNIK, AXIN2 and cMYC at the protein level. NCB-0846 showed 6.8-fold higher cell growth-inhibitory activity against HCT116 cells than NCB-0970. Meanwhile, compared with NCB-0970, NCB-0846 showed much higher (~20-fold) inhibitory activity against colony formation by the same cells in soft agar , indicating that this compound has more potent activity against the clonogenicity of cancer cells. NCB-0846 was administrable orally and suppressed the growth of tumours established by inoculating HCT116 cells into immunodeficient mice. The body weight of mice fell at the beginning of NCB-0846 administration, but gradually recovered.

NVP-CGM097 (CGM-097) |MDM2 inhibitor

NVP-CGM097 (CGM-097) |MDM2 inhibitor

NVP-CGM097 (CGM-097) is a potent and selective MDM2 inhibitor.

Product Name: NVP-CGM097 (CGM-097)|Cat No. DC9769|CAS: 1313363-54-0|Other names:CGM097; CGM-097; CGM 097; NVPCGM097; NVPCGM 097; NVPCGM-097|MW: 659.26|Molecule Formular: C38H47ClN4O4 |Purity>98%.

CGM097 is an orally bioavailable HDM2 (human homolog of double minute 2) antagonist with potential antineoplastic activity. Upon oral administration, p53/HDM2 interaction inhibitor CGM097 inhibits the binding of the HDM2 protein to the transcriptional activation domain of the tumor suppressor protein p53. By preventing this HDM2-p53 interaction, the proteosome-mediated enzymatic degradation of p53 is inhibited, which may result in the restoration of p53 signaling and, thus, the p53-mediated induction of tumor cell apoptosis. HDM2, a zinc finger nuclear phosphoprotein, is a negative regulator of the p53 pathway, often overexpressed in cancer cells and has been implicated in cancer cell proliferation and survival.

A-1155463|A1155463| BCL-XL inhibitor

A-1155463|A1155463| BCL-XL inhibitor

A-1155463 is a highly potent and selective BCL-XL inhibitor.

Product Name: A1155463|Cat No. DC9768|CAS: 1235034-55-5|Other names:A-1155463; A 1155463; A1155463.|MW: 669.79|Molecule Formular: C35H32FN5O4S2 |Purity>98%

A-1155463 is a highly potent and selective BCL-XL inhibitor. A-1155463 is substantially more potent against BCL-XL-dependent cell lines relative to WEHI-539, while possessing none of its inherent pharmaceutical liabilities. A-1155463 caused a mechanism-based and reversible thrombocytopenia in mice and inhibited H146 small cell lung cancer xenograft tumor growth in vivo following multiple doses. A-1155463 thus represents an excellent tool molecule for studying BCL-XL biology as well as a productive lead structure for further optimization.

SHR-1977|SHR1977|ROMK/hERG inhibitor

SHR-1977|SHR1977|ROMK/hERG inhibitor

SHR-1977 is a novel ROMK/hERG inhibitor, (ROMK IC50 = 44 nM, hERG IC50 = >100,000 nM)

Product Name: SHR-1977|Cat No. DC9767|CAS: N/A|Other names:SHR1977,SHR 1977|MW: 419.44|Molecule Formular: C21H21N7O3|Purity>98%

SHR-1977 (ROMK IC50 = 44 nM, hERG IC50 = >100,000 nM) displayed a linear exposure relationship with dose in rats and dogs. SHR-1977 also showed selectivity for ROMK over other inward-rectifier potassium ion channels. In rats, diuresis and natriuresis were increased with oral doses of 0.3 mg/kg (3.88- and 3.25-fold, respectively, compared to vehicle) and 1.0 mg/kg (4.77- and 2.92-fold, respectively, compared to vehicle). In spontaneously hypertensive rats, daily mean systolic blood pressure was significantly reduced by these doses given for 3 days.

LY3177833|LY-3177833|CDC7 inhibitor

LY3177833|LY-3177833|CDC7 inhibitor

LY3177833 is a novel CDC7 inhibitor,CDC7/DBF4 IC50 = 3.3 nM, pMCM2 (S53) IC50 = 290 nM and IVTI TEC70 = 1.6 mcM.

Product Name: LY3177833|Cat No. DC9766|CAS: 1627696-51-8|Other names:LY 3177833,LY-3177833|MW: 309.3|Molecule Formular: C16H12FN5O|Purity>98%

LY3177833 is a novel CDC7 inhibitor,CDC7/DBF4 IC50 = 3.3 nM, pMCM2 (S53) IC50 = 290 nM and IVTI TEC70 = 1.6 mcM. LY-3177833 showed MED = 5 mg/kg (p.o.) in vivo. LY-3177833 strongly impacted chromosome dynamics. In mouse xenograft models, broad antitumor activity was associated with robust dose/exposure-dependent in vivo target inhibition. In addition, the preclinical profile of LY-3177833 was different from nonselective CDC7 inhibitors and cytotoxic agents, something that supports its clinical development with a continuos dosing regime

CERC-501(LY-2456302)| DC Chemicals

CERC-501(LY-2456302)| DC Chemicals

CERC-501(LY-2456302) is a potent, selective antagonist of the kappa opioid receptor (KOR) (Ki = 0.81 nM vs. 24.0 nM and 155 nM for the μ-opioid receptor (MOR) and δ-opioid receptor (DOR), respectively.

Product Name: CERC-501(LY-2456302)|Cat No. DC9765|CAS: 1174130-61-0|Other names:LY2456302,LY 2456302|MW: 418.5|Molecule Formular: C26H27FN2O2|Purity>98%

CERC-501 is a potent and selective kappa opioid receptor(KOR) antagonist.

Afoxolaner|cas 1093861-60-9| DC Chemicals

Afoxolaner|cas 1093861-60-9| DC Chemicals

Afoxolaner is an isoxazoline that inhibits insect and acarine ligand-gated chloride channels, in particular those gated by the neurotransmitter gamma-aminobutyric acid (GABA), blocking pre and post synaptic transfer of chloride ions across cell membranes.

Product Name: Afoxolaner|Cat No. DC9764|CAS: 1093861-60-9|Other names:Afoxolaner|MW: 625.87|Molecule Formular: C26H17ClF9N3O3|Purity>98%

Afoxolaner is an isoxazoline that inhibits insect and acarine ligand-gated chloride channels, in particular those gated by the neurotransmitter gamma-aminobutyric acid (GABA), thereby blocking pre- and post- synaptic transfer of chloride ions across cell membranes. It induces hyperexcitation in the nervous system of susceptible insects. This leads to uncontrolled insect nervous system activity and death of insects and acarines.Afoxolaner is selectively toxic to the insect and acarine nervous system due to differential sensitivity for insect and acarine GABA receptors compared to mammalian GABA receptors.

Piboserod (SB 207266)|5-HT(4) receptor antagonist

Piboserod (SB 207266)|5-HT(4) receptor antagonist

Piboserod (SB 207266) is a selective 5-HT(4) receptor antagonist.

Product Name: Piboserod (SB 207266)|Cat No. DC9763|CAS: 152811-62-6|Other names:SB207266,SB-207266,SB 207266|MW: 369.5|Molecule Formular: C22H31N3O2|Purity>98%

Piboserod (SB 207266) is a selective 5-HT(4) receptor antagonist.
Piboserod did not modify the basal contractions but concentration-dependently antagonized the ability of 5-HT to enhance bladder strip contractions to EFS. In presence of 1 and 100 nM of piboserod, the maximal 5-HT-induced potentiations were reduced to 45.0+/-7.9 and 38.7+/-8.7%, respectivel.
Piboserod significantly increased LVEF by 1.7% vs. placebo (CI 0.3, 3.2, P = 0.020), primarily through reduced end-systolic volume from 165 to 158 mL (P = 0.060). There was a trend for greater increase in LVEF (2.7%, CI -1.1, 6.6, P = 0.15) in a small subset of patients not on chronic beta-blocker therapy. There was no significant effect on neurohormones, quality of life, or exercise tolerance. Patients on piboserod reported more adverse events, but numbers were too small to identify specific safety issues. Pretreatment with potent 5-HT4 ligands dose-dependently reduced striatal SB207145 concentration and the effective dose to achieve 50% receptor occupancy (ED50 ) values were 4.8, 2.0, 7.4, 9.9, 3.8 and 0.02mg/kg for GR113808, piboserod, prucalopride, RS67333, TD8954 and PF04995274, respectively.

Emricasan|pan caspase inhibitor

Emricasan|pan caspase inhibitor

Emricasan (IDN-6556, PF-03491390) is a potent irreversible pan-caspase inhibitor.

Product Name: Emricasan|Cat No. DC9762|CAS: 254750-02-2|Other names:IDN 6556; PF 03491390; PF03491390; PF-03491390; IDN-6556,IDN6556,PF03491390|MW: 569.5|Molecule Formular: C26H27F4N3O7|Purity>98%

Emricasan (IDN-6556, PF-03491390) is a potent irreversible pan-caspase inhibitor.
in vitro: Three caspase inhibitors (IDN-8066, IDN-1965, and IDN-6556) effectively attenuated SEC apoptosis and caspase 3 activation. The most potent inhibitor, IDN-6556, reduced SEC apoptosis and caspase 3 activity by 55% and 94%, respectively. Prevention of SEC apoptosis byIDN-6556 was not reduced when this agent was administered only during the cold preservation period.
in vivo: In the mouse alpha-Fas model of liver injury, i.p. administration of IDN-6556 resulted in marked reduction of alanine aminotransferase (ALT), apoptosis, and caspase activities at a dose of 3 mg/kg. At this dose, IDN-6556 was also effective when given up to 2 h before alpha-Fas and as late as 4 h after alpha-Fas administration. In both the alpha-Fas and d-galactosamine/lipopolysaccharide (D-Gln/LPS) model, ED(50) values in the sub-milligram per kilogram range were established after a number of routes of administration (i.p., i.v., i.m., or p.o.), ranging from 0.04 to 0.38 mg/kg [2]. IDN-6556 (20 mg/kg) given for 7 days post-transplant led to a significantly enhanced rate of diabetes reversal as compared to vehicle. In addition, mice receiving caspase inhibitor displayed improved glucose tolerance and graft survival at the 1-month point.


RK-33|RK33|DDX3 inhibitor

RK-33|RK33|DDX3 inhibitor

RK-33 is a novel DDX3 inhibitor for lung cancer therapy.

Product Name: RK-33|Cat No. DC9761|CAS: 1070773-09-9|Other names:RX33, RX 33|MW: 428.16|Molecule Formular: C23H20N6O3|Purity>98%

RK-33 is a novel DDX3 inhibitor for lung cancer therapy. RK-33 binds to DDX3 and abrogates its activity. Inhibition of DDX3 by RK-33 caused G1 cell cycle arrest, induced apoptosis, and promoted radiation sensitization in DDX3-overexpressing cells. Importantly, RK-33 in combination with radiation induced tumor regression in multiple mouse models of lung cancer. Mechanistically, loss of DDX3 function either by shRNA or by RK-33 impaired Wnt signaling through disruption of the DDX3-β-catenin axis and inhibited non-homologous end joining-the major DNA repair pathway in mammalian somatic cells.

For research only, not for human use.

Dihexa (PNB-0408)

Dihexa (PNB-0408)

Dihexa is an oligopeptide drug that binds with high affinity to hepatocyte growth factor (HGF) and potentiates its activity at its receptor, c-Met.

Product Name: Dihexa (PNB-0408)|Cat No. DC9760|CAS: 1401708-83-5|Other names:|MW: 504.67|Molecule Formular: C27H44N4O5|Purity>98%

Dihexa (developmental code name PNB-0408), also known as N-hexanoic-Tyr-Ile-(6) aminohexanoic amide, is an oligopeptide drug derived from angiotensin IV that binds with high affinity to hepatocyte growth factor (HGF) and potentiates its activity at its receptor, c-Met. The compound has been found to potently improve cognitive function in animal models of Alzheimer's disease-like mental impairment.[1][2][3][4][5][6][7][8][9][10] In an assay of neurotrophic activity, Dihexa was found to be seven orders of magnitude more potent than brain-derived neurotrophic factor.

For research only, not for human use.

RO0921|RO-0921|SYK inhibitor

RO0921|RO-0921|SYK inhibitor

RO0921 is a novel, potent SYK inhibitor.

Product Name: RO0921|Cat No. DC9759|CAS: N/A|Other names:RO-0921,RO 0921|MW: 355.44|Molecule Formular: C18H25N7O|Purity>98%

RO0921 is a novel, potent SYK inhibitor.RO0921 (compound-19) displayed excellent levels of efficacy, inhibiting arthritis scores in a dose-dependent manner at the dose range 5−45 mg/kg by as much as 64% (45 mg/kg, once a day), an efficacy that is comparable to that of

For research only, not for human use.

NI-57|NI57|BRPF BRD inhibitor

NI-57|NI57|BRPF BRD inhibitor

NI-57 is a potent inhibitor of the bromodomains of BRPF proteins that binds to BRPF1B, BRPF2, and BRPF3 with Kd values of 31, 108, and 408 nM, respectively, as determined by isothermal titration calorimetry.

Product Name: NI-57|Cat No. DC9758|CAS: N/A|Other names:NI57,NI 57|MW: 383.4|Molecule Formular: C19H17N3O4S|Purity>98%

The bromodomain and PHD finger-containing (BRPF) proteins are scaffolding components of chromatin-binding MOZ/MORF histone acetyltransferase complexes, which have activity as transcriptional regulators.BRPF1 (BR140 or Peregrin) is important for maintaining Hox gene expression and the development of multiple tissues, axial skeleton, and the hematopoietic system.NI-57 is a potent inhibitor of the bromodomains of BRPF proteins that binds to BRPF1B, BRPF2, and BRPF3 with Kd values of 31, 108, and 408 nM, respectively, as determined by isothermal titration calorimetry. It is selective for BRPFs over other bromodomains. NI-57 shows accelerated FRAP recovery at 1 µM in the BRPF2 FRAP assay, preventing binding of full-length BRPF2 to chromatin.

For research only, not for human use.

CCF642|CCF-642|PD1 inhibitor

CCF642|CCF-642|PD1 inhibitor

CCF642 is a novel protein disulfide isomerases (PDI) inhibitor.

Product Name: CCF642|Cat No. DC9757|CAS: 346640-08-2|Other names:CCF 642,CCF-642|MW: 377.98|Molecule Formular: C15H10N2O4S3|Purity>98%

CCF642, a bone marrow-sparing compound, exhibited a submicromolar IC50 in 10 of 10 multiple myeloma cell lines. An active biotinylated analog of CCF642 defined binding to the PDI isoenzymes A1, A3, and A4 in MM cells. In vitro, CCF642 inhibited PDI reductase activity about 100-fold more potently than the structurally distinct established inhibitors PACMA 31 and LOC14. Computational modeling suggested a novel covalent binding mode in active-site CGHCK motifs. Remarkably, without any further chemistry optimization, CCF642 displayed potent efficacy in an aggressive syngeneic mouse model of multiple myeloma and prolonged the lifespan of C57BL/KaLwRij mice engrafted with 5TGM1-luc myeloma, an effect comparable to the first-line multiple myeloma therapeutic bortezomib. Consistent with PDI inhibition, CCF642 caused acute ER stress in multiple myeloma cells accompanied by apoptosis-inducing calcium release.

For research only, not for human use.

IMR-1|IMR1|CAS 310456-65-6

IMR-1|IMR1|CAS 310456-65-6

IMR-1 Inhibits the Notch Transcriptional Activation Complex to Suppress Tumorigenesis.

Product Name: IMR-1|Cat No. DC9756|CAS: 310456-65-6|Other names:eFT 508,eFT-508|MW: 353.04|Molecule Formular: C15H15NO5S2|Purity>98%

IMR-1 disruptS the recruitment of Mastermind-like 1 to the Notch transcriptional activation complex on chromatin, thereby attenuating Notch target gene transcription. Furthermore, IMR-1 inhibited the growth of Notch-dependent cell lines and significantly abrogated the growth of patient-derived tumor xenografts.

For research only, not for human use.

eFT508|eFT-508|MKNK1/2 protein inhibitor

eFT508|eFT-508|MKNK1/2 protein inhibitor

eFT508 is a MKNK1/2 protein inhibitor..

Product Name: eFT508|Cat No. DC9755|CAS: 1849590-01-7|Other names:eFT 508,eFT-508|MW: 340.38|Molecule Formular: C17H20N6O2|Purity>98%

eFT508 is an orally bioavailable, first-in-class, inhibitor of mitogen-activated protein kinase (MAPK)-interacting serine/threonine-protein kinase 1 (MNK1) and 2 (MNK2), with potential antineoplastic activity. Upon oral administration, MNK1/2 inhibitor eFT508 binds to and inhibits the activity of MNK1 and 2. This prevents MNK1/2-mediated signaling, and inhibits the phosphorylation of certain regulatory proteins, including eukaryotic translation initiation factor 4E (eIF4E), that regulate the translation of messenger RNAs (mRNAs) involved in tumor cell proliferation, angiogenesis, survival and immune signaling. This inhibits tumor cell proliferation in MNK1/2-overexpressing tumor cells. MNK1/2 are overexpressed in a variety of tumor cell types and promote phosphorylation of eIF4E; eIF4E is overexpressed in many tumor cell types and contributes to tumor development, maintenance and resistance.

For research only, not for human use.

NT157|NT-157|inhibitor of IRS-1/2

NT157|NT-157|inhibitor of IRS-1/2

NT157 is a selective inhibitor of IRS-1/2,  IC50 values at sub-micromolar doses (ranging from 0.3 to 0.8 μM) .

Product Name: NT-157|Cat No. DC9754|CAS: 1384426-12-3|Other names:NT157,NT 157|MW: 412.26|Molecule Formular: C16H14BrNO5S|Purity>98%

NT157 significantly affects the cells' migratory ability, as confirmed by a wound-healing assay. NT157 induces cytostatic effects, as evidenced by G2/M cell cycle arrest, and does not affect apoptosis. NT157, a novel small-molecule that specifically targets IRS protein, in OS cells. NT157 is a small-molecule inhibitor that induces Ser-phosphorylation and consequently the degradation of IRS-1 and IRS-2. NT157 efficiently affects migration ability of MG-63 and U-2OS OS cells. NT157 treatment induces cell cycle arrest and inhibits IGF system signaling. [1] The density of LNCaP cells grown in FBS was decreased approximately 20% at 1 μM, approximately 70% at 2 μM, and >90% at 5 μM (IC50, 1.4 μM). Growth of LNCaP cells is suppressed >60% when cultured in CSS but still exhibited significant density at 2 μM and maximal decreased density at 5 μM. The density of FBS-cultured PC3 cells was similarly decreased by NT157 treatment (40% at 2 μM and > 70% at 5 μM; IC50, 2.5 μM).
in vivo: NT157 suppresses growth of LNCaP xenografts following castration. NT157 treatment affects IGF1R and IRS targets in xenografts and significantly delays castration-resistant progression of LNCaP androgen-responsive xenografts when combined with castration. NT157 potentiates docetaxel activity in PC3 xenografts.


For research only, not for human use.

FCCP|uncoupler of oxidative phosphorylation

FCCP|uncoupler of oxidative phosphorylation

FCCP is a very potent uncoupler of oxidative phosphorylation in mitochondria.

Product Name: FCCP|Cat No. DC9753|CAS: 370-86-5|Other names:|MW: 254.17|Molecule Formular: C10H5F3N4O|Purity>98%

Potent mitochondrial oxidative phosphorylation uncoupler (IC50 = 20 nM). Disrupts ATP synthesis by transporting protons across mitochondrial inner membranes. Depolarises mitochondrial membrane potential.

For research only, not for human use.

PHCCC|CAS 179068-02-1

PHCCC|CAS 179068-02-1

PHCCC is a Group I metabotropic glutamate receptor antagonist (IC50 ~ 3 μM).

Product Name: PHCCC|Cat No. DC9752|CAS: 179068-02-1|Other names:|MW: 294.31|Molecule Formular: C17H14N2O3|Purity>98%

PHCCC is a Group I metabotropic glutamate receptor antagonist (IC50 ~ 3 μM).Also a positive allosteric modulator for mGlu4a; potentiates L-AP4-mediated inhibition of striatopallidal synaptic transmission in vitro. Displays antiParkinsonian effects in rats in vivo.

For research only, not for human use.

Velpatasvir(GS5816)|HCV/NS5A inhibitor

Velpatasvir(GS5816)|HCV/NS5A inhibitor

Velpatasvir(GS-5816) is a potent and selective Hepatitis C virus NS5A inhibitor.

Product Name: Velpatasvir(GS5816)|Cat No. DC9751|CAS: 1377049-84-7|Other names:GS 5816,GS-5816|MW: 882.4|Molecule Formular: C49H54N8O8|Purity>98%

Velpatasvir, also known as GS-5816, is a potent and selective Hepatitis C virus NS5A inhibitor. GS-5816 has demonstrated pan-genotypic activity and a high barrier to resistance in HCV replicon assays. GS-5816 demonstrated pangenotypic antiviral activity in patients with genotype 1-4 HCV infection. It will be further evaluated in combination with other pangenotypic direct-acting antivirals to achieve the goal of developing a well-tolerated, highly effective treatment for all HCV genotypes.

For research only, not for human use.


Bexagliflozin (EGT1442)|SGLT2 inhibitor

Bexagliflozin (EGT1442)|SGLT2 inhibitor

Bexagliflozin (EGT1442) is a potent and selective SGLT2 inhibitor, attenuates blood glucose and HbA1c levels in db/db mice and prolongs the survival of stroke-prone rats.

Product Name: Bexagliflozin (EGT1442)|Cat No. DC9750|CAS: 1118567-05-7|Other names:EGT 1442,EGT-1442|MW: 464.94|Molecule Formular: C24H29ClO7|Purity>98%

For research only, not for human use.

Halofuginone|cas 55837-20-2

Halofuginone|cas 55837-20-2

Halofuginone is the competitively inhibitor of prolyl-tRNA synthetase with Ki of 18.3 nM.It could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng/ml in mammal.

Product Name: Halofuginone|Cat No. DC9749|CAS: 55837-20-2|Other names:|MW: 414.68|Molecule Formular: C16H17BrClN3O3|Purity>98%

For research only, not for human use.

PIK-III|cas 1383716-40-2

PIK-III|cas 1383716-40-2

PIK-III, which is a selective inhibitor of ​VPS34 enzymatic activity, inhibits autophagy and de novo lipidation of LC3 and leads to the stabilization of autophagy substrates.

Product Name: PIK-III|Cat No. DC9747|CAS: 1383716-40-2|Other names:|MW: 319.36|Molecule Formular: C17H17N7|Purity>98%

For research only, not for human use.

RSL3|cas 1219810-16-8

RSL3|cas 1219810-16-8RSL3|cas 1219810-16-8

RSL3 is a ferroptosis activator in a VDAC-independent manner,exhibiting selectivity for tumor cells bearing oncogenic RAS.

Product Name: RSL3|Cat No. DC9746|CAS: 1219810-16-8|Other names:RSL 3,RSL-3|MW: 440.88|Molecule Formular: C23H21ClN2O5|Purity>98%

For research only, not for human use.

PD0166285|cas 185039-89-8

PD0166285|cas 185039-89-8

PD0166285 is a potent Wee1 and Chk1 inhibitor with activity at nanomolar concentrations.PD0166285 is a novel G2 checkpoint abrogator.

Product Name: PD0166285|Cat No. DC9744|CAS: 185039-89-8|Other names:PD 0166285,PD-0166285|MW: 512.43|Molecule Formular: C26H27Cl2N5O2|Purity>98%

For research only, not for human use.

CB1954(Tretazicar) |cas 21919-05-1

CB1954(Tretazicar) |cas 21919-05-1

CB1954(Tretazicar) is a anticancer prodrug that is converted in the presence of the enzyme NQO2 and co-substrate caricotamide ( EP-0152R) (EP) into a potent cytotoxic bifunctional alkylating agent.It can be activated by NAD(P)H quinone oxidoreductase 2.

Product Name: CB1954(Tretazicar) |Cat No. DC9743|CAS: 21919-05-1|Other names:CB 1954,CB-1954|MW: 252.18|Molecule Formular: C9H8N4O5|Purity>98%

For research only, not for human use.

Ponesimod|cas 854107-55-4

Ponesimod|cas 854107-55-4

Ponesimod(ACT-128800) is an orally active, selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator with EC50 of 5.7 nM.

Product Name: Ponesimod|Cat No. DC9742|CAS: 854107-55-4|Other names:|MW: 460.97|Molecule Formular: C23H25ClN2O4S|Purity>98%

For research only, not for human use.

Mad2 inhibitor-1 (M2I-1)|cas 312271-03-7

Mad2 inhibitor-1 (M2I-1)|cas 312271-03-7

Mad2 Inhibitor-1 (M2I-1) is a small molecule protein-protein interaction inhibitor targeting the mitotic spindle assembly checkpoint.

Product Name: Mad2 inhibitor-1 (M2I-1)|Cat No. DC9741|CAS: 312271-03-7|Other names:M2I1,M2I 1,M2I-1|MW: 404.48|Molecule Formular: C19H24N4O4S|Purity>98%

Mad2 inhibitor-1 (M2I-1) is the first small molecule inhibitor targeting the binding of Mad2 to Cdc20, an essential protein-protein interaction (PPI) within the SAC. M2I-1 disturbs conformational dynamics of Mad2 critical for complex formation with Cdc20. Cellular studies revealed that M2I-1 weakens the SAC response, indicating that the compound might be active in cells.

For research only, not for human use.

CFI-402257|CFI402257|TTK inhibitor

CFI-402257|CFI402257|TTK inhibitor

CFI-402257 is a highly potent and selective TTK (threonine tyrosine kinase) Inhibitor ((TTK Ki = 0.1 nM) with potential anticancer activity.

Product Name: CFI402257|Cat No. DC9740|CAS: 1610759-22-2|Other names:CFI402257,CFI 402257,CFI-402257 |MW: 497.2|Molecule Formular: C29H31N5O3|Purity>98%

CFI-402257 is a highly potent and selective TTK (threonine tyrosine kinase) Inhibitor ((TTK Ki = 0.1 nM) with potential anticancer activity. TTK is an essential chromosomal regulator and is overexpressed in aneuploid tumors. High TTK levels correlate with a high tumor grade11 and poor patient outcomes. TTK inhibition are associated with a disabled mitotic checkpoint, resulting in chromosome segregation errors, aneuploidy, and cell death.

For research only, not for human use.

ReACp53 |Inhibitor of p53 Aggregation

ReACp53 |Inhibitor of p53 Aggregation

ReACp53 is a cell-penetrating peptide,designed to inhibit p53 amyloid formation.

Product Name: ReACp53(TFA salt)|Cat No. DC9739|CAS: N/A|Other names:RRRRRRRRRRPILTRITLE|MW: 2617.12|Molecule Formular: C108H206N52O24|Purity>98%

ReACp53 is a cell-penetrating peptide,designed to inhibit p53 amyloid formation, rescues p53 function in cancer cell lines and in organoids derived from high-grade serous ovarian carcinomas (HGSOC), an aggressive cancer characterized by ubiquitous p53 mutations.

For research only, not for human use.

GSK2881078|androgen receptor modulator(SARM)

GSK2881078|androgen receptor modulator(SARM)

GSK2881078 (GSK-2881078 ) is a selective androgen receptor modulator (SARM).

Product Name: GSK2881078|Cat No. DC9738|CAS: 1539314-06-1|Other names:GSK 2881078,GSK-2881078|MW: 330.33|Molecule Formular: C14H13NF3N2O2S|Purity>98%

GSK2881078 is a selective androgen receptor modulator (SARM) that is being evaluated for effects on muscle growth and strength in subjects with muscle wasting to improve their physical function.

For research only, not for human use.

SHP099,SHP-099|SHP2 inhibitor

SHP099,SHP-099|SHP2 inhibitor

SHP099 is a selective, orally bioavailable, and efficacious SHP2 inhibitor with IC50 =0.07 μM and p-ERK modulation in cells IC50 = 0.250 μM.

Product Name: SHP099 hydrochloride |Cat No. DC9737|CAS: 1801747-11-4|Other names:SHP099,SHP 099,SHP-099|MW: 388.72|Molecule Formular: C16H20Cl3N5|Purity>98%

SHP099 is a potent, selective, orally bioavailable, and efficacious SHP2 inhibitor with IC50 =0.07 μM and p-ERK modulation in cells IC50 = 0.250 μM. SHP099 exhibits dose-dependent pathway inhibition and antitumor activity in xenograft models. SHP-099 stabilizes SHP2 in an auto-inhibited conformation, concurrently binds to the interface of the N-terminal SH2, C-terminal SH2, and protein tyrosine phosphatase domains, thus inhibiting SHP2 activity through an allosteric mechanism. SHP099 suppresses RAS–ERK signaling to inhibit the proliferation of receptor-tyrosine-kinase-driven human cancer cells in vitro and is efficacious in mouse tumor xenograft models. SHP099’s activity provides evidence that pharmacological inhibition of SHP2 is a viable strategy to target RTK-driven cancers and presents a new chemical tool for further interrogation of the multifaceted cellular functions of SHP2 in development, tumorigenesis, RTK-driven drug resistance and immune-checkpoint modulation.SHP2 is a nonreceptor protein tyrosine phosphatase (PTP) encoded by the PTPN11 gene involved in cell growth and differentiation via the MAPK signaling pathway. SHP2 also purportedly plays an important role in the programmed cell death pathway (PD-1/PD-L1). Because it is an oncoprotein associated with multiple cancer-related diseases, as well as a potential immunomodulator, controlling SHP2 activity is of significant therapeutic interest.

For research only, not for human use.

CPI1189(REN-1189)|CAS 183619-38-7

CPI1189(REN-1189)|CAS 183619-38-7

CPI-1189 prevents apoptosis and reduces glial fibrillary acidic protein immunostaining in a TNF-alpha infusion model for AIDS dementia complex.

Product Name: CPI1189(REN-1189)|Cat No. DC9736|CAS: 183619-38-7|Other names:CPI-1189,CPI 1189,REN1189,REN 1189|MW: 234.14|Molecule Formular: C13H18N2O2|Purity>98%

For research only, not for human use.

SB-366791,SB366791|TRPV1 antagonist

SB-366791,SB366791|TRPV1 antagonist

SB-366791 is a selective and competitive VR1 (TRPV1) antagonist that is commonly used in pain research.

Product Name: SB-366791|Cat No. DC9735|CAS: 472981-92-3|Other names:SB 366791,SB366791|MW: 287.74|Molecule Formular: C16H14NO2Cl|Purity>98%

SB-366791 is a selective and competitive VR1 (TRPV1) antagonist that is commonly used in pain research. The vanilloid recepter type 1 (VR1) is a non-selective cation channel gated by capsaicin, noxious heat, and protons. VR1 is present in primary sensory neurons and in both central and peripheral sensory nerve terminals.

For research only, not for human use.

NS-1619,NS1619| MaxiKα activator

NS-1619,NS1619| MaxiKα activator

NS-1619 is a selective MaxiKα (large conductance calcium activated potassium channel) activator.

Product Name: NS-1619|Cat No. DC9734|CAS: 153587-01-0|Other names:NS1619,NS 1619|MW: 362.23|Molecule Formular: C15H8F6N2O2|Purity>98%

NS-1619 is a selective MaxiKα (large conductance calcium activated potassium channel) activator. In neutrophils, NS-1619 activation of BKCa channels increased alkalinization of phagocytic vacuoles.

For research only, not for human use.

GSK583,GSK-583| RIP2K inhibitor

GSK583,GSK-583| RIP2K inhibitor

GSK583 is a Highly Potent and Selective Inhibitor of RIP2 Kinase (RIP2K bing IC50=5 nM; rat in vivo PD IC50 = 50 nM).

Product Name: GSK-583|Cat No. DC9733|CAS: 1346547-00-9|Other names:GSK 583,GSK583|MW: 398.12|Molecule Formular: C20H19FN4O2S |Purity>98%

For research only, not for human use.

Sufugolix(TAK-013)| GnRHR antagonist

Sufugolix(TAK-013)| GnRHR antagonist

Sufugolix(TAK-013) is a non-peptide, orally-active, selective antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (IC50 = 0.1 and 0.06 nM for

Product Name: Sufugolix(TAK-013)|Cat No. DC9732|CAS: 308831-61-0|Other names:TAK013,TAK 013|MW: 667.724|Molecule Formular: C36H31F2N5O4S|Purity>98%

For research only, not for human use.

2016年10月7日星期五

AZD1283,AZD-1283| P2Y12 receptor inhibitor

AZD1283,AZD-1283| P2Y12 receptor inhibitor

AZD1283 is a potent antagonist of the P2Y12 receptor with EC50 of 3.0 ug/kg/min, TI >10; with binding IC50 of 11 nM.

Product Name: AZD1283|Cat No. DC9731|CAS: 919351-41-0|Other names:AZD-1283,AZD 1283|MW: 470.54|Molecule Formular: C23H26N4O5S|Purity>98%

AZD1283 dose-dependently induced increases in blood flow and inhibition of ADP-induced platelet aggregation with antithrombotic ED50 values of 3.0 and 10 μg/kg/min, respectively. The doses that induced a larger than 3-fold increase in bleeding time were 33 and 100 μg/kg/min for 3 and 13, respectively. Thus, the therapeutic index (TI) was ≥10 for both compounds. On the basis of these data, compound 3 was progressed into human clinical trials as candidate drug AZD1283.

For research only, not for human use.

IC-261(SU-5607)|CK1 inhibitor

IC-261(SU-5607)|CK1 inhibitor

IC261 is a novel inhibitor of CK1, triggers the mitotic checkpoint control. The IC50 of IC261 for CK1 was 16 μM and for Cdk5 is 4.5 mM.

Product Name: IC-261(SU-5607)|Cat No. DC9730|CAS: 186611-52-9|Other names:IC261,SU5607,IC 261,SU 5607|MW: 311.33|Molecule Formular: C18H17NO4|Purity>98%

 IC261 is a specific inhibitor of the protein kinases casein kinase 1-delta and -epsilon, triggers the mitotic checkpoint and induces p53-dependent postmitotic effects. At low micromolar concentrations IC261 inhibits cytokinesis causing a transient mitotic arrest. IC261 selectively inhibits CK1 compared to other protein kinases by an ATP-competitive mechanism.

For research only, not for human use.


Valrocemide (TV1901)

Valrocemide (TV1901)

Product Name: Valrocemide (TV1901,VGD))|Cat No. DC9729|CAS: 92262-58-3|Other names:|MW: 200.278|Molecule Formular: C10H20N2O2|Purity>98%

For research only, not for human use.

Anticonvulsant 7903|cas 82351-05-1

Anticonvulsant 7903|cas 82351-05-1

Product Name: Anticonvulsant 7903|Cat No. DC9728|CAS: 82351-05-1|Other names:Lvguidingan,3,4-dichlorophenyl propenylisobutylamide|MW: 272.17|Molecule Formular: C13H15Cl2NO|Purity>98%

For research only, not for human use.

CP21 (CP21R7)|CAS 125314-13-8 | inhibitor

CP21 (CP21R7)|CAS 125314-13-8 | inhibitor

Product Name: CP21 (CP21R7)|Cat No. DC9726|CAS: 125314-13-8|Other names:|MW: 317.34|Molecule Formular: C19H15N3O2|Purity>98%

For research only, not for human use.