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Biological Activity for MS 436
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.
Sold under license from Icahn School of Medicine at Mount Sinai.
Technical Data for MS 436
|Storage||Store at -20°C|
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.
Solubility Data for MS 436
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for MS 436
The following data is based on the product molecular weight 383.42. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.61 mL||13.04 mL||26.08 mL|
|5 mM||0.52 mL||2.61 mL||5.22 mL|
|10 mM||0.26 mL||1.3 mL||2.61 mL|
|50 mM||0.05 mL||0.26 mL||0.52 mL|
References for MS 436
References are publications that support the biological activity of the product.
Zhang et al (2013) Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains. J.Med.Chem. 56 9251 PMID: 24144283
Segura et al (2013) BRD4 sustains melanoma proliferation and represents a new target for epigenetic therapy. Cancer Res. 73 6264 PMID: 23950209
If you know of a relevant reference for MS 436, please let us know.
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Keywords: MS 436, MS 436 supplier, MS436, potent, selective, BRD4, BrD1, Bromodomain, inhibitors, inhibits, BrD2, gene, transcription, transcriptional, epigenetics, BRD4(1), Bromodomains, 5173, Tocris Bioscience
Citations for MS 436
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
Epigenetics Research Bulletin
Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:
- DNA Methyltransferases
- Histone Deacetylases
- Histone Demethylases
- Histone Methyltransferases
Epigenetics in Cancer Poster
Adapted from the 2015 Cancer Product Guide Edition 3, this poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
Rheumatoid Arthritis Poster
Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.