BSJ-4-116

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BSJ-4-116 是一种高效、选择性 CDK12 降解剂 (PROTAC)，IC50 为 6 nM。它通过提前终止转录（主要是通过增加聚腺苷酸化）来下调 DDR 基因。

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).

BSJ-4-116 (10-10000 nM; 72 hours) exhibits potent antiproliferative effects in Kelly CDK12C1039F.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 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. Cell Proliferation Assay Cell Line:Parental Kelly and CDK12C1039F cellsConcentration:10-10000 nM Incubation Time:72 hours Result:Antiproliferative activity of BSJ-4-116 is independent of the mutational status, and the degrader compounds exhibited improved GR50 (growth rate inhibition) values in Kelly CDK12C1039F cells compared with the parental cell line.Western Blot Analysis Cell Line:Parental and CDK12C1039F (KellyCDK12CF)-expressing Kelly cells Concentration:50?nM Incubation Time:6-24?hours Result:Led to the same level of CDK12 protein level decrease, regardless of the mutational status of the cell line.

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Angiogenesis

CDK

CDK12|Cereblon

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2519823-34-6

837.38

C40H49ClN8O8S

>98% (HPLC)

DMSO:250 mg/mL (298.55 mM; Need ultrasonic)

O=C(NCCCCCCCN1C[C@H](NC2=NC=C(Cl)C(NC3=CC=CC=C3S(=O)(C(C)C)=O)=N2)CCC1)COC4=CC=CC(C(N5C(CC6)C(NC6=O)=O)=O)=C4C5=O

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(-20℃)

With Ice Pack

≥ 2 years