Cat. No. 5173
Chemical Name: (E)-4-[2-(2-Amino-4-hydroxy-5-methy
Biological ActivityPotent 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.
Licensing InformationSold under license from Icahn School of Medicine at Mount Sinai.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Segura et al (2013) BRD4 sustains melanoma proliferation and represents a new target for epigenetic therapy. Cancer Res. 73 6264. PMID: 23950209.
Zhang et al (2013) Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains. J.Med.Chem. 56 9251. PMID: 24144283.
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Keywords: MS 436, supplier, MS436, potent, selective, BRD4, BrD1, Bromodomain, inhibitors, inhibits, BrD2, gene, transcription, transcriptional, epigenetics, BRD4(1), Tocris Bioscience, Bromodomain Inhibitor products
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