MS436|BRD4 inhibitor|CAS# 1395084-25-9

Home >> Signaling Pathways >> Chromatin/Epigenetics >> Bromodomain >> MS436

Size	Price	Stock
10mM (in 1mL DMSO)	$113.00	In stock
5mg	$75.00	In stock
25mg	$243.00	In stock
100mg	$684.00	In stock

Publications citing ApexBio Products

Nature.
2016 Apr 21;532(7599):398-401.

Nature.
2015 Aug 20;524(7565):309-14.

Cell.
2015 Aug 27;162(5):987-1002.

Cell.
2015 Feb 12;160(4):729-44.

Immunity.
2016 Jan 19;44(1):88-102

Nat Cell Biol.
2015 May;17(5):627-38.

Nat Neurosci.
2015 Oct;18(10):1464-73.

Nat Commun.
2016 Feb 1;7:10492.

J Cell Biol.
2016 Apr 11;213(1):109-25.

Cell Host Microbe.
2016 Jul 13;20(1):13-24.

Proc Natl Acad Sci U S A.
2016 Mar 8;113(10):2585-90.

Proc Natl Acad Sci U S A.
2015 Jun 30;112(26):E3365-73.

Proc Natl Acad Sci U S A.
2015 Jul 28;112(30):9412-7.

Autophagy.
2016 Jul 2;12(7):1129-52.

Cancer Res canres.
2946.2015.

Elife.
2016 Jan 14;5. pii: e12203.

Nucleic Acids Res.
2016 Feb 18;44(3):e2.

EMBO Rep.
2015 Sep;16(9):1114-30.

Oncogene.
2016 Mar 21.

Cell Rep.
2015 Sep 29;12(12):1986-96.

Cell Death Differ.
2016 Jun;23(6):1026-37.

Cell Death Differ.
2016 Jan;23(1):76-88.

Diabetes Obes Metab.
2015 Apr;17(4):403-13.

Oncotarget.
2015 Jan 20;6(2):1171-89.

J Neurosci.
2015 Sep 23;35(38):13244-56.

Sci Signal.
2014 Dec 23;7(357):ra122.

Mol Ther.
2015 Sep;23(9):1475-85.

J Nucl Med.
2016 Feb;57 Suppl 1:75S-80S.

Cardiovasc Res.
2015 Apr 1;106(1):153-62.

Cell Mol Life Sci.
2015 Nov;72(22):4399-407.

Anal Chem.
2015;87(10):5046-9.

Cancer Lett.
2016 Apr 28;374(1):1-11.

Quality Control

Quality Control & MSDS

View current batch:

Purity = 98.66%

Chemical structure

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.