I-BET762
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- Application
- Inhibition (Inh)
- Purpose
- BET Bromodomain inhibitor, Suppresses Myc transcription
- Characteristics
- 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 = 32.5nM, BRD3 = 42.4nM, BRD4 = 36.1nM. It was able to suppress proinflammatory proteins by macrophage, block acute inflammation in mice, and suppressed the inflammatory function of T cells. Inhibition of BET bromodomains results in downregulation of Myc transcription, an important oncogene.
- Purity
- >98 %
- 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
- Formula
- C22H22ClN5O2
- Solubility
- Soluble in DMSO (up to at least 25 mg/ml) or in Ethanol (up to at least 25 mg/ml)
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- Restrictions
- For Research Use only
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- Format
- Powder
- Precaution of Use
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GHS – Classification
Not a hazardous substance or mixture - Storage
- -20 °C
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- Background
- GSK525762,Epigenetics,Bromodomain,Immunology,Inflammation,Cancer,Posttranslational modification,Chromatin
- Molecular Weight
- 423.90
- CAS-No
- 1260907-17-2
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