CPI-203
CPI-203 is an orally available derivative of triazolothienodiazepine JQ-1; it exhibits no sedative or anxiolytic efficacy and is currently in development as a potential anticancer compound. Like JQ-1, CPI-203 inhibits the BET bromodomain (BRD) family of proteins, including BRD4; inhibition of this protein downregulates Myc expression and IL-6 production in vitro. This compound also inhibits phosphorylation of the carboxyl-terminus domain of RNA polymerase II.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18853749
| Purity |
≥99% |
|---|---|
| Formula |
C19H18ClN5OS |
| Formula Wt. |
399.90 |
| Melting Point |
151.8°C |
| Appearance |
White to off white powder |
King B, Trimarchi T, Reavie L, et al. The ubiquitin ligase FBXW7 modulates leukemia-initiating cell activity by regulating MYC stability. Cell. 2013 Jun 20;153(7):1552-66. PMID: 23791182.
Devaiah BN, Lewis BA, Cherman N, et al. BRD4 is an atypical kinase that phosphorylates serine2 of the RNA polymerase II carboxy-terminal domain. Proc Natl Acad Sci U S A. 2012 May 1;109(18):6927-32. PMID: 22509028.
