MS 436
Chemical Name: (E)-4-[2-(2-Amino-4-hydroxy-5-methylphenyl)diazenyl]-N-2-pyridinylbenzenesulfonamide
Purity: ≥98%
Biological Activity
MS 436 is a potent and selective BRD4 bromodomain inhibitor (Ki = 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 (IC50 values are 3.8 and 4.9 μM, respectively). Attenuates melanoma cell proliferation in vitro.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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BRD4 sustains melanoma proliferation and represents a new target for epigenetic therapy.
Segura et al.
Cancer Res., 2013;73:6264 -
Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains.
Zhang et al.
J.Med.Chem., 2013;56:9251
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