CPI-203isanorallyavailablederivativeoftriazolothienodiazepineJQ-1;itexhibitsnosedativeoranxiolyticefficacyandiscurrentlyindevelopmentasapotentialanticancercompound.LikeJQ-1,CPI-203inhibitstheBETbromodomain(BRD)familyofproteins,includingBRD4;inhibitionofthisproteindownregulatesMycexpressionandIL-6productioninvitro.Thiscompoundalsoinhibitsphosphorylationofthecarboxyl-terminusdomainofRNApolymeraseII.
| Purity | ≥99% |
|---|---|
| Formula | C19H18ClN5OS |
| FormulaWt. | 399.90 |
| MeltingPoint | 151.8°C |
| Appearance | Whitetooffwhitepowder |
| StoreTemp | Ambient |
|---|---|
| ShipTemp | Ambient |
| InfoSheet | C6132InfoSheetPDF |
|---|
KingB,TrimarchiT,ReavieL,etal.TheubiquitinligaseFBXW7modulatesleukemia-initiatingcellactivitybyregulatingMYCstABIlity.Cell.2013Jun20;153(7):1552-66.PMID:23791182.
DevaiahBN,LewisBA,ChermanN,etal.BRD4isanatypicalkinasethatphosphorylatesserine2oftheRNApolymeraseIIcarboxy-terminaldomain.ProcNatlAcadSciUSA.2012May1;109(18):6927-32.PMID:22509028.
