MS 436

Key Product Details

Product Description

MS 436 is a 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 (IC₅₀ values are 3.8 and 4.9 μM, respectively). Attenuates melanoma cell proliferation in vitro.

Licensing Information

Sold under license from Icahn School of Medicine at Mount Sinai.

Product Specifications for MS 436

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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	1.30 mL	2.61 mL
50 mM	0.05 mL	0.26 mL	0.52 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Segura BRD4 sustains melanoma proliferation and represents a new target for epigenetic therapy. Cancer Res. 2013 PMID: 23950209
• Zhang Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains. J.Med.Chem. 2013 PMID: 24144283

Product Documents for MS 436