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I-BET762 | BET Bromodomain inhibitor / Suppresses Myc transcription

I-BET762 (1260907-17-2) is a potent inhibitor of the BET family of bromodomains with no activity at bromodomains BAZ2B, SP140, ATAD2, CREBBO, and PCAF.1,2 IC50’s for H4Ac peptide displacement: BRD2 = 32.5nM, BRD3 = 42.4nM, BRD4 = 36.1nM.1 It was able to suppress proinflammatory proteins by macrophage, block acute inflammation in mice1, and suppressed the inflammatory function of T cells3. Inhibition of BET bromodomains results in downregulation of Myc transcription, an important oncogene.4

References/Citations

1) Nicodeme et al. (2010), Suppression of inflammation by a synthetic histone mimic; Nature 468 1119
2) Mirguet et al. (2013), Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains; J. Med. Chem., 56 7501
3) Bandukwala et al. (2012), Selective inhibition of CD4+ T-cell cytokine production and autoimmunity by BET protein and c-Myc inhibitors; Proc. Natl. Acad. Sci. USA, 109 14532
4) Delmore et al. (2011), BET Bromodomain as a Therapeutic Strategy to Target c-Myc; Cell 146 904

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Catalog#  10-4122-0005

$70.00
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CAS:
1260907-17-2
Catalog Number:
10-4122
Activity:
BET Bromodomain inhibitor / Supresses Myc transcription
Chemical Name:
(4S)- 6-(4-Chlorophenyl)-N-ethyl-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine-4-acetamide
Alternate Names:
GSK525762
Molecular Weight:
423.90
Molecular Formula:
C22H22ClN5O2
Solubility:
Soluble in DMSO (up to at least 25 mg/ml) or in Ethanol (up to at least 25 mg/ml)
Physical Properties:
Tan solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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