BMS-986158 是一种BET抑制剂，在 MDA-MB231 三阴性乳腺癌细胞和 NCI-H211 小细胞肺癌细胞中，对 BET 的IC50分别为 5 和 6.6 nM。

BMS-986158 is a potent BET inhibitor with IC50s of 6.6 and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respectively.

BMS-986158 is an inhibitor of the bromodomain (BRD) and extra-terminal domain (BET) family of proteins, with potential antineoplastic activity. Upon administration, the BET inhibitor BMS-986158 binds to the acetyl-lysine binding site in the BRD of BET proteins. Thereby preventing the interaction between BET proteins and acetylated histones. This disrupts chromatin remodeling and prevents the expression of certain growth-promoting genes. Resulting in an inhibition of tumor cell growth[2].

1800340-40-2

C30H33N5O2

495.62

DMSO:60 mg/ml (121.06 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years