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Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains
LY2886721 is under clinical study
24)13-6-3-11(9-21-13)15(17
5 μM) reverses the bezafibrate-induced enchancement of ALP activity on d 7 in MC3T3-E1 cells
MS023 - PRMT Inhibitor. CAS# 1831110-54-3 0331 Structure-guided design of potent diazobenzeneMS023, CAS No. 1831110 54 3, is a potent, selective and cell permeable type I PRMT inhibitor (catalyzes mono and asymmetric dimethylation of arginine residues) with IC50 of 30 nM, 119 nM, 83 nM, 4 nM and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6 and PRMT8, respectively. It is completely inactive against type II and type III PRMTs, protein lysine methyltransferases and DNA methyltransferases. A crystal structure of PRMT6 in complex with MS023 revealed that