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EPZ-005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM, 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.

June 21, 2017

prudect name : EPZ-005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM, 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.EPZ005687 Synonyms:…

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EMD 1214063 is an inhibitor of MET tyrosine kinase with potential antineoplastic activity. MET tyrosine kinase inhibitor EMD 1214063 selectively binds to MET tyrosine kinase and disrupts MET signal transduction pathways, which may induce apoptosis in tumor cells overexpressing this kinase. The receptor tyrosine kinase MET (also known as hepatocyte growth factor receptor or HGFR), is the product of the proto-oncogene c-Met and is overexpressed or mutated in many tumor cell types; this protein plays key roles in tumor cell proliferation, survival, invasion, and metastasis, and tumor angiogenesis.

prudect name : EMD 1214063 is an inhibitor of MET tyrosine kinase with potential antineoplastic activity. MET tyrosine kinase inhibitor EMD 1214063 selectively binds to MET tyrosine kinase and disrupts…

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E7080 is the most potent dual inhibitor of VEGF-R3 tyrosine kinase (IC50=5.2 nM) as well as VEGF-R2 tyrosine kinase (IC50=4.0 nM) among those small-molecule inhibitors of VEGF-R kinases, such as sunitinib, sorafenib, and CEP-7055. It has been evaluated in vitro (pre-clinical) for anti-cancer effects. E7080 suppresses lymph node and lung metastases of human mammary breast tumor MDA-MB-231 via inhibition of angiogenesis and lymphangiogenesis.

prudect name : E7080 is the most potent dual inhibitor of VEGF-R3 tyrosine kinase (IC50=5.2 nM) as well as VEGF-R2 tyrosine kinase (IC50=4.0 nM) among those small-molecule inhibitors of VEGF-R…

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E-64 is a natural, potent, and irreversible inhibitor of cysteine proteases; IC50 values for inhibiting cathepsins K, S, and L, in vitro, are 1.4, 4.1, and 2.5 nM, respectively.

prudect name : E-64 is a natural, potent, and irreversible inhibitor of cysteine proteases; IC50 values for inhibiting cathepsins K, S, and L, in vitro, are 1.4, 4.1, and 2.5…

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maraviroc(CAS NO:376348-65-1)intermediates

prudect name : maraviroc(CAS NO:376348-65-1)intermediatesethyl 4,4-difluorocyclohexanecarboxylate Synonyms: CAS NO: 178312-47-5Molecular Formula: C9H14F2O2Molecular Weight: 192.20Purity: ≥98%Solubility: Storage: −20°C 2 years APO866 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18512135

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Elvitegravir inhibits PBMC and PA with IC50 of 0.89 and 20 nM, respectively. Elvitegravir prevents the integration of HIV-1 cDNA through the inhibition of DNA strand transfer. Elvitegravir suppresses the replication of HIV-1, including various subtypes and multiple-drug-resistant clinical isolates, and HIV-2 strains with a 50% effective concentration in the subnanomolar to nanomolar range. Elvitegravir inhibits the replication of HIV-1 clinical isolates carrying NRTI, NNRTI, and PI resistance-associated genotypes. Elvitegravir inhibits the HIV replication at a step that occurs after reverse transcription but before proteolytic cleavage, consistent with the integration step. Elvitegravir inhibits the synthesis of strand transfer products with an IC50 of 54 nM. Elvitegravir blocks integration via the inhibition of IN-mediated strand transfer. Elvitegravir inhibits the integration of the HIV-based vector used as a positive control for the luciferase assay with an EC50 of 0.8 nM, as observed in the MAGI assay with HIV-1IIIB. Elvitegravir suppresses the replication of MLV infection with IC50 of 5.8 nM as well as that of the primate retrovirus SIV (IC50 = 0.5 nM), revealing that IN inhibitors have antiviral activity against a broad range of retroviruses. EVG is active against HIV-1 and HIV-2 and has a serum-free antiviral IC50 of 0.3-0.9 nM in peripheral blood mononuclear cells.

prudect name : Elvitegravir inhibits PBMC and PA with IC50 of 0.89 and 20 nM, respectively. Elvitegravir prevents the integration of HIV-1 cDNA through the inhibition of DNA strand transfer….

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Sunitinib(CAS NO:557795-19-4)Intermediates

prudect name : Sunitinib(CAS NO:557795-19-4)Intermediatesethyl 2,4-dimethyl-1H-pyrrole-3-carboxylate Synonyms: CAS NO: 2199-51-1Molecular Formula: C9H13NO2Molecular Weight: 167.21Purity: ≥98%Solubility: Storage: −20°C 2 years ABT627 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18511946

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Entinostat (MS-275, SNDX-275) is a potent HDAC inhibitor with IC50 of 0.3 and 8µM for HDAC1 and HDAC3, respectively. Entinostat (MS-275, SNDX-275) is synthetic benzamide derivative with potential antineoplastic activity. Entinostat (MS-275, SNDX-275) has no inhibitory activity towards HDAC8 (IC50>100 µM). Entinostat (MS-275, SNDX-275) appears to exert dose-dependent effects in human leukemia cells at low concentrations in human prostate cancer cell lines. Entinostat (MS-275, SNDX-275) exerted growth arrest in PC-3 and LNCaP cells, and induced cell death in DU-145 cells.

prudect name : Entinostat (MS-275, SNDX-275) is a potent HDAC inhibitor with IC50 of 0.3 and 8µM for HDAC1 and HDAC3, respectively. Entinostat (MS-275, SNDX-275) is synthetic benzamide derivative with…

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EMD534085 is a kinesin inhibitor currently in clinical development.

prudect name : EMD534085 is a kinesin inhibitor currently in clinical development.EMD 534085 Synonyms: CAS NO: 858668-07-2Molecular Formula: C25H31F3N4O2Molecular Weight: 476.53Purity: 98% minSolubility: In DMSOStorage: −20°C 2 years BIBF1120 References…

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Inhibitor of Wnt signaling. Induces an increase in Axin2 protein levels; promotes ¦Â-catenin phosphorylation by stabilizing Axin-scaffolded destruction complexes. Negative control exo-IWR (Cat. No. 3947) available.

prudect name : Inhibitor of Wnt signaling. Induces an increase in Axin2 protein levels; promotes ¦Â-catenin phosphorylation by stabilizing Axin-scaffolded destruction complexes. Negative control exo-IWR (Cat. No. 3947) available.endo-IWR 1…

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