Roscovitine (TAK 165) is a potent EGFR and p34cdc2 inhibitor with IC50 of 6 nM and 0.2 µM, respectively. Roscovitine (TAK 165) also inhibits p33cdk2 and p33cdk5.Roscovitine (TAK 165) displays > 4000-fold selectivity over EGFR, FGFR, PDGFR, JAK1 and Src. Roscovitine (TAK 165) exhibits potent antiproliferative effects in ErbB2-overexpressing cancer cell lines (IC50 = 5 nM in BT474 breast cancer cells) and significantly inhibits bladder, breast and prostate cancer xenograft growth in vivo.

June 21, 2017

prudect name : Roscovitine (TAK 165) is a potent EGFR and p34cdc2 inhibitor with IC50 of 6 nM and 0.2 µM, respectively. Roscovitine (TAK 165) also inhibits p33cdk2 and p33cdk5.Roscovitine…

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MK-2048 is a second generation integrase inhibitor, intended to be used against HIV infection.

prudect name : MK-2048 is a second generation integrase inhibitor, intended to be used against HIV infection.MK-2048 Synonyms: CAS NO: 870005-19-9Molecular Formula: C21H21ClFN5O4 Molecular Weight: 461.9 Purity: 98% minSolubility: In…

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Chemical Name: N¡¯-[(3Z)-1-Hexyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene]benzohydrazide

prudect name : Chemical Name: N¡¯-[(3Z)-1-Hexyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene]benzohydrazideMDA 19 Synonyms: CAS NO: 1048973-47-2Molecular Formula: C21H23N3O2Molecular Weight: 349.43Purity: 98% minSolubility: In DMSOStorage: −20°C web site: www.medchemexpress.com References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18524992

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Chemical Name: 3,5-Di-tert-butyl-4-hydroxybenzylidenemalononitrile

prudect name : Chemical Name: 3,5-Di-tert-butyl-4-hydroxybenzylidenemalononitrileMalonoben Synonyms: CAS NO: 10537-47-0Molecular Formula: C18H22N2OMolecular Weight: 282.38Purity: 98% minSolubility: In DMSOStorage: −20°C web site: www.medchemexpress.com References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18524989

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Linagliptin shows a potent inhibition effect against DPP-4 in vitro and a low affinity for hERG channel and M1 receptor (IC50 295 nM). Linagliptin acts as a competitive inhibitor with a Ki of 1 nM, and also shows 10,000-fold more selectivity for DPP-4 than DPP-8, DPP-9, amino-peptidases N and P, prolyloligopeptidase, trypsin, plasmin, and thrombin, and 90-fold more selectivity than fibroblast activation protein in vitro.

prudect name : Linagliptin shows a potent inhibition effect against DPP-4 in vitro and a low affinity for hERG channel and M1 receptor (IC50 295 nM). Linagliptin acts as a…

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LH846 is a selective inhibitor of CK1¦Ä (IC50 values are 290 nM, 1.3 uM and 2.5 uM for CK1¦Ä, ¦Å and ¦Á); displays no inhibitory activity at CK2.

prudect name : LH846 is a selective inhibitor of CK1¦Ä (IC50 values are 290 nM, 1.3 uM and 2.5 uM for CK1¦Ä, ¦Å and ¦Á); displays no inhibitory activity at…

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LY315920(Varespladib) is a selective inhibitor of human, group IIA, nonpancreatic secretory PLA2 (sPLA2). In a chromogenic isolated enzyme assay, Varespladib inhibited sPLA2 activity with an IC50 of 9.6 ¡À1 nM or 7.3 ¡Á10-6 mole fraction, which approached the stiochiometric limit of this assay.

prudect name : LY315920(Varespladib) is a selective inhibitor of human, group IIA, nonpancreatic secretory PLA2 (sPLA2). In a chromogenic isolated enzyme assay, Varespladib inhibited sPLA2 activity with an IC50 of…

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Selective inhibitor of TGF-¦Â type-I receptor (TGF-¦Â RI, TGFR-I, T¦ÂR-I, ALK-5) (IC50 values are 59, 400 and 1400 nM for TGR-¦Â RI, TGF-¦Â RII and MLK-7K respectively). Inhibits TGF-¦Â-dependent luciferase production in mink lung cells (p3TP lux) and growth in mouse fibroblasts (NIH 3T3) (IC50 values are 47 and 89 nM respectively). Suppresses invasion of MDA-MB-231 breast cancer cells in a matrigel invasion assay.

prudect name : Selective inhibitor of TGF-¦Â type-I receptor (TGF-¦Â RI, TGFR-I, T¦ÂR-I, ALK-5) (IC50 values are 59, 400 and 1400 nM for TGR-¦Â RI, TGF-¦Â RII and MLK-7K respectively)….

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LY3009120 is a small molecule that has been shown in vitro to be a pan-RAF inhibitor of all isoforms, blocking proliferation in both BRAF and RAS mutant cells.

prudect name : LY3009120 is a small molecule that has been shown in vitro to be a pan-RAF inhibitor of all isoforms, blocking proliferation in both BRAF and RAS mutant…

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2-Butyl-4-chloro-1-[2¡¯-(1H-tetrazol-5-yl)biphenyl-4-ylmethyl]imidazole-5-carboxylic acid

prudect name : 2-Butyl-4-chloro-1-[2¡¯-(1H-tetrazol-5-yl)biphenyl-4-ylmethyl]imidazole-5-carboxylic acidLOSARTAN CARBOXYLIC ACID Synonyms: CAS NO: 124750-92-1Molecular Formula: C22H21ClN6O2Molecular Weight: 436.89Purity: 98% minSolubility: DMSOStorage: -20¡æ web site: www.medchemexpress.com References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18524894

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