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Dot1L-IN-1
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-1图片
CAS NO:2088518-50-5

Dot1L-IN-1是高效,选择性,结构新颖的Dot1L抑制剂,Ki为2pM。
Cas No.2088518-50-5
Canonical SMILESCC1=NC=CC=C1C2=C(Cl)SC3=CC=C(NC(NCC(NCCCN(C)[C@@H]4CCCN(C5=C(C=CN6)C6=NC=N5)C4)=O)=O)C=C32
分子式C32H36ClN9O2S
分子量646.21
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-1 is a highly potent, selective and structurally novel Dot1L inhibitor with a Ki of 2 pM.

Dot1L-IN-1 potently suppresses H3K79 dimethylation (IC50 = 3 nM), the direct product of the Dot1Lcatalyzed reaction, as well as the activity of the HoxA9 promoter (IC50 = 17 nM) in HeLa and Molm-13 cells, respectively[1]. Dot1L-IN-1 effectively inhibits proliferation of the human MLL-rearranged leukemia cell line MV4-11 carrying the oncogenic MLL-AF4 fusion (IC50 = 5 nM)[1].

[1]. M?bitz H, et al. Discovery of Potent, Selective, and Structurally Novel Dot1L Inhibitors by a Fragment Linking Approach. ACS Med Chem Lett. 2017 Feb 14;8(3):338-343.

 
 
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