YKL-5-124

Description: YKL-5-124, a potent, selective and covalent CDK7 inhibitor with an IC50 of 9.7 nM, 1300 nM and 3020 nM for CDK7/Mat1/CycH, CDK2 and CDK9 respectively, displays biochemical and cellular selectivity for CDK7 over CDK12/13. Target: CDK. Smiles: CN(C)C[C@@H](NC(=O)N1Cc2c(NC(=O)c3ccc(NC(=O)C=C)cc3)n[nH]c2C1(C)C)c1ccccc1. References: Olson CM, Liang Y, Leggett A, Park WD, Li L, Mills CE, Elsarrag SZ, Ficarro SB, Zhang T, Düster R, Geyer M, Sim T, Marto JA, Sorger PK, Westover KD, Lin CY, Kwiatkowski N, Gray NS. Development of a Selective CDK7 Covalent Inhibitor Reveals Predominant Cell-Cycle Phenotype. Cell Chem Biol. 2019 Jun 20,26(6):792-803.e10.