BET bromodomain inhibitor. Downregulates Myc expression, causes G1cell cycle arrest and attenuates cell proliferation in human pancreatic neuroendocrine tumors. Arrests the growth of T cell acute lymphoblastic leukemia cellsin vitro(EC50= 91.2 nM). Also e
Storage Temp
Store at 2-8°C
Shipped In
Wet ice
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of bromodomain containing 4
Product Description
CPI203 is a potent BET bromodomain inhibitor with IC50 of 37 nM for BRD4.
Associated Targets(Human)
BRD4TchemBromodomain-containing protein 4 (2 Activities)
1.Moros A, Rodríguez V, Saborit-Villarroya I, Montraveta A, Balsas P, Sandy P, Martínez A, Wiestner A, Normant E, Campo E et al.. (2014) Synergistic antitumor activity of lenalidomide with the BET bromodomain inhibitor CPI203 in bortezomib-resistant mantle cell lymphoma.. Leukemia, 28 (10):(2049-59). [PMID:24721791][10.1021/op500134e]
2.Wong C, Laddha SV, Tang L, Vosburgh E, Levine AJ, Normant E, Sandy P, Harris CR, Chan CS, Xu EY. (2014) The bromodomain and extra-terminal inhibitor CPI203 enhances the antiproliferative effects of rapamycin on human neuroendocrine tumors.. Cell Death Dis, 5 (13):(e1450). [PMID:25299775][10.1021/op500134e]
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F2002054