化学性质:
规格 | 250mg 500mg |
CAS | 2088518-50-5 |
别名 | N/A |
化学名 | N/A |
分子式 | C32H36ClN9O2S |
分子量 | 646.21 |
溶解度 | Soluble in DMSO |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
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.
特别提醒:
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标签:Dot1L-IN-1
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