BSJ-4-116,2519823-34-6

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BSJ-4-116

CAS No. : 2519823-34-6

MCE 国际站：BSJ-4-116

产品活性：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。

研究领域：PROTAC  |  Cell Cycle/DNA Damage

作用靶点：PROTACs  |  CDK

In Vitro: BSJ-4-116 (10-10000 nM; 72 hours) exhibits potent antiproliferative effects in Kelly CDK12^C1039F.
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^C1039F 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.

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