Takeda compound 101
Cat. No.: DC11955
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Chemical Structure
865608-11-3
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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. |
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