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Submit ReviewMS 436
Description: Potent and selective BRD4(1) inhibitor
Chemical Name: (E)-4-[2-(2-Amino-4-hydroxy-5-methylphenyl)diazenyl]-N-2-pyridinylbenzenesulfonamide
Purity: ≥98% (HPLC)
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.
Licensing Information
Sold under license from Icahn School of Medicine at Mount Sinai.
Technical Data for MS 436
| M. Wt | 383.42 |
| Formula | C18H17N5O3S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1395084-25-9 |
| PubChem ID | 60171585 |
| InChI Key | BBJDRANVVNBXAR-JWGURIENSA-N |
| Smiles | NC1=C(/N=N/C2=CC=C(S(NC3=NC=CC=C3)(=O)=O)C=C2)C=C(C)C(O)=C1 |
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 | |
|---|---|---|---|
| Solubility | |||
| DMSO | 38.31 | 100 |
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 |
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Product Datasheets for MS 436
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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