YKL-5-124 是选择性不可逆CDK7共价抑制剂，对CDK7和CDK7/Mat1/CycH的IC50分别为 53.5 nM 和 9.7 nM。它诱导强烈的细胞周期停滞，并抑制 E2F 驱动的基因表达。它对 CDK7 的生化和细胞选择性优于 CDK12/13。它对CDK7的选择性比 CDK9 和 CDK2 高 100 倍以上。

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.

1957203-01-8

C28H33N7O3

515.61

DMSO:220 mg/mL (426.68 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years