MS 436

Pricing Availability   Qty
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)
Datasheet
Citations
Reviews
Literature (5)

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.

Select a batch to recalculate based on the batch molecular weight:
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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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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Reviews for MS 436

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Literature in this Area

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