MS436, BRD4 Inhibitor

MS436 is a potent and selective BET bromodomain inhibitor with Ki of <0.085 μM and 0.34 μM for BRD4 (1) and BRD4 (2), respectively. It effectively inhibits BRD4 activity in NF-κB-directed production of nitric oxide and proinflammatory cytokine interleukin-6 in murine macrophages without siginificanty inhibition on cell viability. MS436 represents a new class of bromodomain inhibitors to study the functional differences of the two bromodomains of BRD4

Product information

CAS Number: 1395084-25-9

Molecular Weight: 383.42

Formula: C18H17N5O3S

Chemical Name: (E)-4-((2-amino-4-hydroxy-5-methylphenyl)diazenyl)-N-(pyridin-2-yl)benzenesulfonamide

Smiles: CC1=CC(/N=N/C2C=CC(=CC=2)S(=O)(=O)NC2=CC=CC=N2)=C(N)C=C1O

InChiKey: DZTGIRNXWSZBIM-QURGRASLSA-N

InChi: InChI=1S/C18H17N5O3S/c1-12-10-16(15(19)11-17(12)24)22-21-13-5-7-14(8-6-13)27(25,26)23-18-4-2-3-9-20-18/h2-11,24H,19H2,1H3,(H,20,23)/b22-21+

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

MS436 was used at 10-100 µM final concentration in various in vitro assays.

References:

1. Zhang G, et al. Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains. (2013) J Med Chem. 56(22):9251-64.

Products are for research use only. Not for human use.