I-BET762 | BET Bromodomain inhibitor / Suppresses Myc transcription
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $80.00 | ||
| 25 mg | $295.00 |
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
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
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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