BMS-986158,1800340-40-2

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BMS-986158

CAS No. : 1800340-40-2

MCE 国际站：BMS-986158

产品活性：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。

研究领域：Epigenetics

作用靶点：Epigenetic Reader Domain

In Vitro: 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.

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