Chemical Name: N-[(1S)-2-(Dimethylamino)-1-phenylethyl]-4,6-dihydro-6,6-dimethyl-3-[[4-[(1-oxo-2-propen-1-yl)amino]benzoyl]amino]pyrrolo[3,4-c]pyrazole-5(1H)-carboxamide
Biological ActivityYKL-5-124 is a potent and selective CDK7/Mat1/CycH and cyclin dependent kinase (CDK7) inhibitor (IC50 values = 9.7 nM and 53.5 nM, respectively). YKL-5-124 shows 100-fold selectivity over CDK9 and CDK2. YKL-5-124 induces cell cycle arrest at the G1/S transition, inhibits E2F-driven gene expression and inhibits CDK1 and CDK3 T-loop phosphorylation.
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