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Dot1L-IN-2
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。
Dot1L-IN-2图片
CAS NO:1940206-71-2
包装与价格：
包装价格(元)
250mg电议
500mg电议

产品介绍
Dot1L-IN-2是一种有效的，选择性的，可口服的Dot1L(一种histonemethyltransferase)，IC50值和Ki值分别为0.4nM和0.08nM。
Cas No.1940206-71-2
Canonical SMILESCN1C=NC2=CC(OC3=CC=CC=C3N4C(C)=CC5=C4C=C(NC6=NC=CC(NC)=N6)C=C5)=CN=C21
分子式C27H24N8O
分子量476.53
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Dot1L-IN-2 is a potent, selective and orally bioavailable inhibitor of Dot1L (a histone methyltransferase), with an IC50 and Ki of 0.4 nM and 0.08 nM, respectively.

Dot1L-IN-2 is a potent, selective Dot1L inhibitor, with an IC50 and Ki of 0.4 nM and 0.08 nM, respectively. Dot1L-IN-2 potently inhibits H3K79 dimethylation (IC50, 16 nM), and blocks the activity of the HoxA9 promoter (IC50, 340 nM) in cellular systems. Dot1L-IN-2 also dramatically suppresses proliferation of the human MLL-rearranged leukemia cell line MV4-11 carrying the oncogenic MLL-AF4 fusion (IC50, 128 nM)[1].

[1]. Chen C, et al. Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach. ACS Med Chem Lett. 2016 Jun 1;7(8):735-40.