Toggle Nav
APExBIO

MS436

In stock
Catalog No.
B1012
BRD4 inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$113.00
In stock
5mg
$75.00
In stock
25mg
$243.00
In stock
100mg
$684.00
In stock

Tel: +1-832-696-8203

Email: sales@apexbt.com

Worldwide Distributors

MS436 is a potent and selective small-molecule inhibitor of BRD4 with Ki values of <0.085μM and 0.34μM, respectively for BrD1 and BrD2 [1].

BRD4 plays a role in gene transcription and is a drug target for cancer and inflammation. It has two bromodomains. MS436 is a diazobenzene compound, it is designed from the SAR studies to have higher selectivity. In vitro fluorescent anisotropy assay shows MS436 has about 10-fold higher affinity of BrD1 over BrD2. MS436 binds to BRD4 through a set of water-mediated interaction and this is the molecular basis for the binding affinity. MS436 also has activity to CBP BrD. In RAW264.7 cells, MS436 can block NF-κB-directed NO production and block the expression of proinflammatory cytokine interleukin (IL)-6 induced by LPS [1].

References:
[1] Zhang G, Plotnikov AN, Rusinova E, Shen T, Morohashi K, Joshua J, Zeng L, Mujtaba S, Ohlmeyer M, Zhou MM. Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains. J Med Chem. 2013 Nov 27;56(22):9251-64.

Physical Appearance

A solid

Chemical Properties

StorageStore at -20°C
M.Wt383.42
Cas No.1395084-25-9
FormulaC18H17N5O3S
Solubility≥19.15mg/mL in DMSO
Chemical Name4-[(2Z)-2-(2-amino-5-methyl-4-oxocyclohexa-2,5-dien-1-ylidene)hydrazinyl]-N-pyridin-2-ylbenzenesulfonamide
SDFDownload SDF
Canonical SMILESCC1=CC(=NNC2=CC=C(C=C2)S(=O)(=O)NC3=CC=CC=N3)C(=CC1=O)N
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description MS436 is a potent and selective small-molecule inhibitor of BRD4 with Ki values of <0.085 μM and 0.34 μM for BrD1 and BrD2, respectively .
Targets BrD1 BrD2        
IC50 <0.085 μM 0.34 μM        

Quality Control

Chemical structure

MS436