I-BET762

I-BET762 is a potent inhibitor of the BET family of bromodomains with no activity at bromodomains BAZ2B, SP140, ATAD2, CREBBO, and PCAF. IC50’s for H4Ac peptide displacement: BRD2=32.5 nM, BRD3=42.4nM, BRD4=36.1nM. It was able to suppress key inflammatory genes as well as the release of proinflammatory cytokines and prevent acute inflammation in mice. Suppresses the inflammatory function of T cells. Inhibition of BET bromodomains results in downregulation of Myc transcription, an important oncogene.

Catalog ID: CV-1036-1

$133.00

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  • Product Details
    • Size: 5.0 mg
    • Physical State: Tan powder
    • Temperature Storage: -20°C
    • Temperature Shipping: Ambient
    • Molecular Mass: 423.9

  • References

    1. Nicodeme, E., et al., (2010) Nature, 468 : 1119
    2. Mirguet, O., et al., (2013) J. Med. Chem., 56 : 7501
    3. Bandukwala, H.S., et al., (2012) Proc. Natl. Acad. Sci. USA, 109 : 14532
    4. Delmore, J.E., et al., (2011) Cell, 146 : 904

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