BSJ-4-116 是一种高效的选择性 CDK12 降解剂,IC50 为 6 nM,是由Cereblon配体和CDK配体相连的 PROTAC。它通过提前终止转录来下调 DDR 基因,主要是通过增加聚腺苷酸化,具有抗增殖作用。
产品描述
BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. It downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation).
体外活性
BSJ-4-116 (50?nM; 6-24?hours) decreases the level of CDK12 protein, regardless of the mutational status of the cell line.BSJ-4-116 (10-10000 nM; 72 hours) exhibits potent antiproliferative effects in Kelly CDK12C1039F.BSJ-4-116 inhibits the growth of T-ALL cells (Jurkat and MOLT-4 cells) and sensitizes them to PARP inhibition. BSJ-4-116 regulates DDR genes via poly(adenylation). BSJ-4-116 overcomes CDK12C1039F mutation. BSJ-4-116 represents the first example of resistance to a bivalent degrader molecule that is a consequence of an acquired point mutation in the target protein.
Cas No.
2519823-34-6
分子式
C40H49ClN8O8S
分子量
837.39
别名
BSJ-4-116
储存和溶解度
DMSO:250 mg/mL (298.55 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years