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MS436BRD4 inhibitor

MS436

Catalog No. B1012
Size Price Stock Qty
10mM (in 1mL DMSO) $113.00 In stock
5mg $75.00 In stock
25mg $243.00 In stock
100mg $684.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Quality Control & MSDS

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Chemical structure

MS436

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        

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Chemical Properties

Cas No. 1395084-25-9 SDF Download SDF
Chemical Name 4-[(2Z)-2-(2-amino-5-methyl-4-oxocyclohexa-2,5-dien-1-ylidene)hydrazinyl]-N-pyridin-2-ylbenzenesulfonamide
Canonical SMILES CC1=CC(=NNC2=CC=C(C=C2)S(=O)(=O)NC3=CC=CC=N3)C(=CC1=O)N
Formula C18H17N5O3S M.Wt 383.42
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For 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.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

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.