BMS-986158 |
| カタログ番号GC32812 |
BMS-986158 は、NCI-H211 小細胞肺がん (SCLC) 細胞および MDA-MB231 トリプルネガティブ乳がん (TNBC) 細胞でそれぞれ 6.6 および 5 nM の IC50 を持つ強力な BET 阻害剤です。
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Cas No.: 1800340-40-2
Sample solution is provided at 25 µL, 10mM.
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BMS-986158 is an inhibitor of the bromodomain and extra-terminal (BET) proteins.
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].
[1]. von Schaper E. Roche bets on bromodomains. Nat Biotechnol. 2016 Apr;34(4):361-2. [2]. BET Inhibitor BMS-986158.
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