CHF 114.00
In stock
SYN-3033-M0011 mgCHF 114.00
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Product Details
Synonyms GSK-525762A
Product Type Chemical
Formula C22H22ClN5O2
MW 423.9
CAS 1260907-17-2
Purity Chemicals ≥95%
Appearance Solid.
Solubility Soluble in DMSO.
Declaration Manufactured by SynKinase.
Other Product Data Target: BRD2, BRD3, and BRD4 | 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
I-BET762 (GSK525762A) is an inhibitor for BET (bromodomain and extra terminal domain) proteins, BRD2, BRD3 and BRD4. It binds to the tandem bromodomains of BET with a Kd of 50.5-61.3nM, displaces a tetra-acetylated H4 peptide prebound to tandem bromodomains of BET with IC50 of 32.5-42.5nM in FRET analysis. I-BET762 disrupts the formation of the chromatin complexes essential for expression of inflammatory genes.
Product References
  1. Suppression of inflammation by a synthetic histone mimic: E. Nicodeme, et al.; Nature 468, 1119 (2010)
  2. Selective inhibition of CD4+ T-cell cytokine production and autoimmunity by BET protein and c-Myc inhibitors: H.S. Bandukwala, et al.; PNAS 109, 14532 (2012)
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