MS436 |
Catalog No.GC13148 |
MS436은 브로모도메인 억제제의 새로운 부류로, BRD4 BrD1에 대해 추정된 Ki=30-50nM의 강력한 친화도 및 BrD2에 대해 10배 선택성을 나타냅니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1395084-25-9
Sample solution is provided at 25 µL, 10mM.
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.
Average Rating: 5
(Based on Reviews and 13 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *