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SGC 0946
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SGC 0946图片
CAS NO:1561178-17-3
规格:98%
分子量:618.57
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
DOT1L inhibitor,highly potent and selective
CAS:1561178-17-3
分子式:C28H40BrN7O4
分子量:618.57
纯度:98%
存储:Store at -20°C

Background:

SGC 0946 is a potent small-molecule inhibitor of protein methyltransferase (PMT) DOT1L, a unique protein lysine methyltransferase (PKMT) catalyzing the methylation of histone H3 on Lysine 79 (H3K79), with the half maximal inhibition concentration IC50 value of 0.3 nM [1].


As a brominated analogue of EPZ004777, SGC 0946 exhibits substantially increased cellular inhibitory potency than its predecessor, where SGC 0946 reduces the methylation of H3K79 in both MCF10A (IC50: 8.8 nM) and A431 (IC50: 2.65 nM) cells compared with EPZ004777 (IC50: 84 nM and 264 nM respectively). This greatly increased cellular inhibitory potency of SGC 0946 can be attributed to lower off-rate and to improved cell permeability [1].


Reference


参考文献:
[1] Yu W, Chory EJ, Wernimont AK, Tempel W, Scopton A, Federation A, Marineau JJ, Qi J, Barsyte-Lovejoy D, Yi J, Marcellus R, Iacob RE, Engen JR, Griffin C, Aman A, Wienholds E, Li F, Pineda J, Estiu G, Shatseva T, Hajian T, Al-Awar R, Dick JE, Vedadi M, Brown PJ, Arrowsmith CH, Bradner JE, Schapira M. Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat Commun. 2012;3:1288. doi: 10.1038/ncomms2304.