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

BMS-986158 is a potent BET inhibitor with IC 50 s 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.

Solid

IC50: 6.6 nM (BET, in NCI-H211 SCLC cells), 5?nM (in MDA-MB231 TNBC) cells)

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. 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]. Yin M, et al. Potent BRD4 inhibitor suppresses cancer cell-macrophage interaction. Nat Commun. 2020 Apr 14;11(1):1833.

In Vitro: DMSO : 50 mg/mL (100.88 mM; Need ultrasonic)H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)配制储备液