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BSJ-4-116
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BSJ-4-116图片
CAS NO:2519823-34-6
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
500 mg电议

产品介绍
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