CPI 203

Biological Activity

CPI 203 is a 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 (EC₅₀ = 91.2 nM). Also enhances the antitumor effect of rapamycin (Cat. No. 1292) in vitro and attenuates rapamycin induced Akt activation. Also enhances fibroblast reprogramming to hiPSCs at low concentration. Orally bioavailable.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. 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
2. The ubiquitin ligase FBXW7 modulates leukemia-initiating cell activity by regulating MYC stability.
   King et al.
   Cell, 2013;153:1552
3. Reprogramming by de-bookmarking the somatic transcriptional program through targeting of BET bromodomains.
   Shao et al.
   Cell Rep., 2016;16:3138

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