Dot1L-IN-2

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Dot1L-IN-2 

Dot1L-IN-2 是一种有效的,选择性的,可口服的 Dot1L (一种 histone methyltransferase),IC50 值和 Ki 值分别为 0.4 nM 和 0.08 nM。

Dot1L-IN-2

Dot1L-IN-2 Chemical Structure

CAS No. : 1940206-71-2

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生物活性

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.

IC50 & Target

IC50: 0.4 nM (Dot1L)[1]
Ki: 0.08 nM (Dot1L)[1]

体外研究
(In Vitro)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

476.53

Formula

C27H24N8O

CAS 号

1940206-71-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [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.

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