Chemical Name: N-[(1,2-Dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[6-(4-methyl-1-piperazinyl)-3-pyridinyl]-1H-pyrazolo[3,4-b]pyridine-4-carboxamide
Biological ActivityPotent and selective SAM-competitive EZH2 lysine methyltransferase inhibitor (IC50 = 11 nM). Selectively binds EZH2 over a panel of 22 methyltransferases. Reduces global level of the PRC2-associated mark H3K27me3 in K562 cells. Suppresses cell growth in CML cells. Inhibits colony formation of primary human CD34+ CML stem/ progenitor cells. Antitumor effects in vivo.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Chronic myelogenous leukemia- initiating cells require polycomb group protein EZH2.
Xie et al.
Send to, 2016;6:1237
Developing EZH2-targeted therapy for lung cancer.
Frankel et al.
Cancer Discov., 2016;6:949
Oncogenic deregulation of EZH2 as an opportunity for targeted therapy in lung cancer.
Zhang et al.
Cancer Discov., 2016;6:1006
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