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MS436

现货
Catalog No.
B1012
BRD4抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,130.00
现货
5mg
¥ 750.00
现货
25mg
¥ 2,430.00
现货
100mg
¥ 6,840.00
现货

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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.

Chemical Properties

Physical AppearanceA solid
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
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

生物活性

描述 MS436是BRD4的一个有效的、选择性小分子抑制剂,Ki值<0.085 μM。对BRD1和BRD2抑制的Ki值为0.34 μM。
靶点 BrD1 BrD2        
IC50 <0.085 μM 0.34 μM        

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