Dot1L-IN-1 TFA is a highly potent and selective Dot1L inhibitor with a K i of 2 pM and an IC 50 of <0.1 nM. Dot1L-IN-1 TFA potently suppresses H3K79 dimethylation (IC 50 =3 nM), as well as the activity of the HoxA9 promoter (IC 50 =17 nM) in HeLa and Molm-13 cells, respectively.
性状
Solid
IC50 & Target[1][2]
DOT1L
体外研究(In Vitro)
Dot1L-IN-1 (analogue 7) TFA effectively inhibits proliferation of the human MLL-rearranged leukemia cell line MV4-11 carrying the oncogenic MLL-AF4 fusion (IC50=5 nM). has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 50 mg/mL (65.77 mM; Need ultrasonic)配制储备液
[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.