BET bromodomain inhibitor. Downregulates Myc expression, causes G1
cell cycle arrest and attenuates cell proliferation in human pancreatic neuroendocrine tumors. Arrests the growth of T cell acute lymphoblastic leukemia cells in vitro
= 91.2 nM). Also enhances the antitumor effect of rapamycin
(Cat. No. 1292) in vitro
and attenuates rapamycin induced Akt activation. Orally bioavailable.
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The bromodomain and extra-terminal inhibitor CPI203 enhances the antiproliferative effects of rapamycin on human neuroendocrine tumors.
Wong et al.
Cell Death Dis., 2014;5:e1450
The ubiquitin ligase FBXW7 modulates leukemia-initiating cell activity by regulating MYC stability.
King et al.