化学性质:
规格 | 10mM (in 1mL DMSO) 5mg 25mg 100mg |
CAS | 1395084-25-9 |
别名 |
|
化学名 | 4-[(2Z)-2-(2-amino-5-methyl-4-oxocyclohexa-2,5-dien-1-ylidene)hydrazinyl]-N-pyridin-2-ylbenzenesulfonamide |
分子式 | C18H17N5O3S |
分子量 | 383.42 |
溶解度 | ≥ 19.15mg/mL in DMSO |
储存条件 | 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. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
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].
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标签:MS436
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