Inhibitor of BET proteins
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I-BET762

Item No. 10676

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(S)-2-(6-(4-chlorophenyl)-8-methoxy-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-N-ethylacetamide
CAS Number
1260907-17-2
Synonyms
  • GSK525762A
Molecular Formula
C22H22ClN5O2
Formula Weight
423.9
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 20 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH 7.2) (1:1): 0.5 mg/ml
SMILES
COC1=CC(C(C2=CC=C(Cl)C=C2)=N[C@H]3CC(N(CC)[H])=O)=C(N4C3=NN=C4C)C=C1
InChi Code
InChI=1S/C22H22ClN5O2/c1-4-24-20(29)12-18-22-27-26-13(2)28(22)19-10-9-16(30-3)11-17(19)21(25-18)14-5-7-15(23)8-6-14/h5-11,18H,4,12H2,1-3H3,(H,24,29)/t18-/m0/s1
InChi Key
AAAQFGUYHFJNHI-SFHVURJKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Cayman Chemical
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    Product Description

    The bromodomain and extra terminal domain (BET) family of proteins, including BRD2, BRD3, and BRD4, affect inflammatory gene expression by controlling the assembly of histone acetylation-dependent chromatin complexes.1,2 I-BET762 is a synthetic compound which interacts with BET proteins with high-affinity (Kd = 32.5-42.5 nM).3,4 It blocks binding of BET proteins with acetylated histones, disrupting the formation of chromatin complexes involved in the expression of specific inflammatory genes in activated macrophages.3 Through these actions, I-BET762 provides protection against bacteria-induced sepsis and lipopolysaccharide-triggered endotoxic shock.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. LeRoy, G., Rickards, B., and Flint, S.J. The double bromodomain proteins Brd2 and Brd3 couple histone acetylation to transcription. Mol. Cell 30(1), 51-60 (2008).

    2. Hargreaves, D.C., Horng, T., and Medzhitov, R. Control of inducible gene expression by signal-dependent transcriptional elongation. Cell 138(1), 129-145 (2009).

    3. Nicodeme, E., Jeffrey, K.L., Schaefer, U., et al. Suppression of inflammation by a synthetic histone mimic. Nature 468(7327), 1119-1123 (2010).

    4. Dawson, M.A., Kouzarides, T., and Huntly, B.J. Targeting epigenetic readers in cancer. N. Engl. J. Med. 367(7), 647-657 (2012).