Description
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: ≥12 months 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:
- 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.
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