BMS-986158

Names

[ CAS No. ]:
1800340-40-2

[ Name ]:
BMS-986158

Biological Activity

[Description]:

BMS-986158 is an inhibitor of the bromodomain and extra-terminal (BET) proteins.

[Related Catalog]:

Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

Research Areas >> Cancer

[Target]

BET[1]

[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[2].

[References]

[1]. von Schaper E. Roche bets on bromodomains. Nat Biotechnol. 2016 Apr;34(4):361-2.

[2]. BET Inhibitor BMS-986158.

[Related Small Molecules]

(+)-JQ1 | GSK126 | Tazemetostat (EPZ-6438) | Birabresib (OTX015) | A 485 | Curcumin | ARV-771 | ARV-825 | I-BET762 | BI 2536 | GSK343 | C646 | 3-Deazaneplanocin A (hydrochloride) | I-BET151 | 666-15

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₀H₃₃N₅O₂

[ Molecular Weight ]:
495.62

[ Storage condition ]:
2-8℃

Related Compounds

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