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SYN-3004-M100100 mgINQ
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Product Details
Product Type Chemical
Formula C23H25ClN4O2S
MW 457.0
CAS 1268524-70-4
Purity Chemicals ≥95%
Appearance Solid.
Solubility Soluble in DMSO or ethanol.
Declaration Manufactured by SynKinase.
Other Product Data Target: BET bromodomain | Kinase Group: N/A | Substrate: N/A
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
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Product Specification Sheet
Datasheet Download PDF
(+)-JQ1 is a potent, high affinity, selective BET bromodomain inhibitor (IC(50) values of 17.7, 32.6, 76.9 and 12942nM respectively for BRD2 (N-terminal (N)), BRD4 (C-terminal (C)), BRD4 (N) and CREBBP, respectively. In binding assays, (+)-JQ1 binds competitive with acetyl lysine to BRD4 bromodomain 1 (Kd=50nM) and and BRD4 bromodomain 2 (Kd=90 nM). May be a useful chemical probe to investigate the role of BET bromodomains in the transcriptional regulation of oncogenesis. (+)-JQ1 exhibited strong dose- and time-dependent inhibition of BRDT, a bromodomain-containing protein highly enriched in testis. BRDT is involved in chromatin remodeling and is essential for healthy sperm development. (+)-JQ1 appears to block that function and causes a decrease in sperm viability, being examined as a potential male contraceptive. Inhibitor of inflammation and bone destruction.
Product References
  1. Selective inhibition of BET bromodomains: P. Filippakopoulos, et al.; Nature 468, 1067 (2010)
  2. BET inhibitor JQ1 blocks inflammation and bone destruction: S. Meng, et al.; J. Dent. Res. 93, 657 (2014)
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