(+)-JQ1 or (+)JQ-1 (CAS: 1268524-70-4)
(+)-JQ1 is a potent and selective inhibitor of BET (bromodomain and extra-terminal) proteins, including BRD2, BRD3, BRD4, and BRDT. It competitively binds to the acetyl-lysine recognition pocket of these proteins, displacing them from chromatin and modulating gene expression.
Key Features:
- High Potency:
- Inhibits BET bromodomains with IC₅₀ values of 77 nM (BRD4 BD1) and 33 nM (BRD4 BD2).
- Selective Action:
- Targets BET family proteins without significantly affecting other bromodomains.
- Reversible Binding:
- Allows controlled modulation of BET activity in research applications.
(+)-JQ1 Applications:
- Cancer Research:
- Investigated for its ability to suppress tumor cell proliferation in cancers like multiple myeloma and leukemia.
- Epigenetic Studies:
- Used as a chemical probe to study BET bromodomain functions in gene regulation.
- Transcriptional Regulation:
- Examines the displacement of BET proteins from chromatin and its effects on gene expression.
(+)JQ-1 is a versatile tool in biomedical research, providing critical insights into BET protein roles in epigenetics, cancer, and transcriptional regulation.
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