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Takeda compound 101

  Cat. No.:  DC11955   Featured
Chemical Structure
865608-11-3
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More than 5000 active chemicals with high quality for research!
Field of application
Compound 101 (GRK2 inhibitor 101, Takeda compound 101, Cmpd101) is a novel membrane-permeable, small-molecule inhibitor of GRK2 and GRK3.
Cas No.: 865608-11-3
Chemical Name: 3-(((4-methyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl)methyl)amino)-N-(2-(trifluoromethyl)benzyl)benzamide
Synonyms: GRK2 inhibitor 101;Takeda compound 101;Cmpd101
SMILES: C(NCC1=CC=CC=C1C(F)(F)F)(=O)C1=CC=CC(NCC2N(C)C(C3C=CN=CC=3)=NN=2)=C1
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Compound 101 (GRK2 inhibitor 101, Takeda compound 101, Cmpd101)is a novel membrane-permeable, small-molecule inhibitor of both GRK2 and GRK3 with IC50s of 18 nM and 5.4 nM. CMPD101 also inhibits ROCK-2 and PKCα (IC50s=1.4 μM and 8.1 μM, respectively)[1].
Target: is a novel membrane-permeable, small-molecule inhibitor of both GRK2 and GRK3 with IC50s of 18 nM and 5.4 nM. CMPD101 also inhibits ROCK-2 and PKCα (IC50s=1.4 μM and 8.1 μM, respectively)[1].
References: [1]. Okawa T, et al. Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure. J Med Chem. 2017 Aug 24;60(16):6942-6990.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
2018-0101
2018-0101
Cat. No. Product name Field of application
DC70442 GRK6 inhibitor 18 GRK6 inhibitor 18 is a potent, and selective GRK6 inhibitor with IC50 of 8 nM.GRK6 inhibitor 18 displays >1,000-fold selectivity over Aurora A, as well as high selectivity against a panel of 85 kinases.GRK6 inhibitor 18 has potent cellular target engagement and antiproliferative activity against MM cells (IC50=0.4-0.46 uM) and is synergistic with bortezomib.
DC11955 Takeda compound 101 Compound 101 (GRK2 inhibitor 101, Takeda compound 101, Cmpd101) is a novel membrane-permeable, small-molecule inhibitor of GRK2 and GRK3.
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