Biological Activity
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.
Compound Libraries
MS 436 is also offered as part of the Tocriscreen Epigenetics Toolbox. Find out more about compound libraries available from Tocris.
Technical Data
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 38.31 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 383.42. Batch specific molecular weights may vary from batch to batch due to solvent 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 |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
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
Keywords: MS 436, supplier, MS436, potent, selective, BRD4, BrD1, Bromodomain, inhibitors, inhibits, BrD2, gene, transcription, transcriptional, epigenetics, BRD4(1), Bromodomains, Bromodomains, Tocris Bioscience
