Dot1L-IN-1是高效，选择性，结构新颖的Dot1L抑制剂，Ki为2pM。
货号:ajcx12910
CAS:2088518-50-5
分子式:C32H36ClN9O2S
分子量：646.21
溶解度:Soluble in DMSO
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.