PFI-1isaninhibitorofBETbromodomains(BRDs)thatpreventstheassociationofBETwithhistones;itactsasanacyl-lysine(Kac)mimeticinhibitor,bindingtheKacsiteofBRD2andBRD4.PFI-1exhibitsanti-inflammatoryandanticanceractivities.InH202-treatedbronchialepithelialcells,PFI-1decreasesexpressionofIL-6andCXCL8.Inleukemiacells,PFI-1downregulatesexpressionofMycandAurKB,inducingG1phasecellcyclearrestandsuppressingcellgrowth.
| CasNo. | 1403764-72-6 |
|---|---|
| Purity | ≥98% |
| Formula | C16H17N3O4S |
| FormulaWt. | 347.39 |
| IUPACName | 2-methoxy-N-(3-methyl-2-oxo-1,4-dihydroquinazolin-6-yl)benzenesulfonamide |
| Synonym | PF-06405761 |
| Appearance | Whitetooffwhitepowder |
| StoreTemp | -20°C |
|---|---|
| ShipTemp | Ambient |
| MSDS | P2133MSDSPDF |
|---|---|
| InfoSheet | P2133InfoSheetPDF |
KhanYM,KirkhamP,BarnesPJ,etal.Brd4IsEssentialforIL-1β-InducedInflammationinHumanAirwayEpithelialCells.PLoSOne.2014Apr23;9(4):e95051.PMID:24759736.
PicaudS,DaCostaD,ThanasopoulouA,etal.PFI-1,ahighlyselectiveproteininteractioninhibitor,targetingBETBromodomains.CancerRes.2013Jun1;73(11):3336-46.PMID:23576556.
