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编 号:F218119
分子式:C30H33N5O2
分子量:495.62
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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生物活性:
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.

体外研究:
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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