MS 436

• Supplier: Tocris Bioscience
• Catalog: 4208
• Prices: $209.00, $879.00
• Sizes: 10 mg, 50 mg
• Function Type: Inhibitor
• Cas Number: 1395084-25-9
• Chemical Name: (E)-4-[2-(2-Amino-4-hydroxy-5-methylphenyl)diazenyl]-N-2-pyridinylbenzenesulfonamide
• Formula: C18H17N5O3S
• Molecular Weight: 383.42
• Purity: >98 %
• Description: Potent and selective BRD4 bromodomain inhibitor (K i = 30 - 50 nM for the first bromodomain (BRD4(1)). Exhibits 10-fold selectivity for BRD4(1) over BRD4(2). Blocks BRD4 transcriptional activity in lipopolysaccharide-induced production of both nitric oxide and IL-6 in mouse macrophages (IC 50 values are 3.8 and 4.9 μ M, respectively). Attenuates melanoma cell proliferation in vitro .

Product References

BRD4 sustains melanoma proliferation and represents a new target for epigenetic - BRD4 sustains melanoma proliferation and represents a new target for epigenetic

Segura MF, Fontanals-Cirera B, Gaziel-Sovran A, Guijarro MV, Hanniford D, Zhang G, Gonzalez-Gomez P, Morante M, Jubierre L, Zhang W, Darvishian F, Ohlmeyer M, Osman I, Zhou MM, Hernando E. Cancer Res. 2013 Oct 15;73(20):6264-76.

Structure-guided design of potent diazobenzene inhibitors for the BET - Structure-guided design of potent diazobenzene inhibitors for the BET

Zhang G, Plotnikov AN, Rusinova E, Shen T, Morohashi K, Joshua J, Zeng L, Mujtaba S, Ohlmeyer M, Zhou MM. J Med Chem. 2013 Nov 27;56(22):9251-64.