Dot1L-IN-2 |
| Catalog No.GC30530 |
Dot1L-IN-2 es un inhibidor potente, selectivo y biodisponible por vÍa oral de Dot1L (una histona metiltransferasa), con una IC50 y una Ki de 0,4 nM y 0,08 nM, respectivamente.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1940206-71-2
Sample solution is provided at 25 µL, 10mM.
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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.
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].
[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.
Average Rating: 5 (Based on Reviews and 17 reference(s) in Google Scholar.)
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