BSJ-4-116 是由 Cereblon 配体和 CDK 配体相连的 PROTAC。BSJ-4-116 是一种高效且选择性的 CDK12 降解剂，IC₅₀ 为 6 nM。BSJ-4-116 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。BSJ-4-116 单独或与聚(ADP-核糖)聚合酶抑制剂 Olaparib (HY-10162) 联合使用时表现出有效的抗增殖作用。

BSJ-4-116 is a PROTAC connected by ligands for Cereblon and CDK. BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC 50 of 6 nM. BSJ-4-116 downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation). BSJ-4-116 exhibits potent antiproliferative effects, alone and in combination with the poly(ADP-ribose) polymerase inhibitor Olaparib (HY-10162).

Solid

CDK12 6 nM (IC50) Cereblon

BSJ-4-116 (10-10000 nM; 72 hours) exhibits potent antiproliferative effects in Kelly CDK12.
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 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 CDK12 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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Jiang B, et al. Discovery and resistance mechanism of a selective CDK12 degrader. Nat Chem Biol. 2021;17(6):675-683.

In Vitro: DMSO : 250 mg/mL (298.55 mM; Need ultrasonic)配制储备液