PIK-75isaninhibitorofp110αPI3Kthatexhibitsanticancerandanti-inflammatoryactivities.Inbreastcancercells,PIK-75inhibitscellmotilityandadhesioninvitroandinvivo.PIK-75alsoenhancesglucose-inducedinsulinsecretion.Additionally,PIK-75inhibitsproductionofTNF-α,IL-6,E-selectin,ICAM-1,andVCAM-1,preventingmonocyte-endothelialcelladhesion.
| CasNo. | 372196-77-5 |
|---|---|
| Purity | ≥98% |
| Formula | C16H14BrN5O4S•HCl |
| FormulaWt. | 488.74 |
| IUPACName | N-[(E)-(6-bromoimidazo[1,2-a]pyridin-3-yl)methylideneamino]-N,2-dimethyl-5-nitrobenzenesulfonamide;hydrochloride |
| Synonym | PIK-75HCl |
| MeltingPoint | 221-223°C |
| Solubility | SolubleinDMSO,DMF |
| Appearance | YellowPowder |
| StoreTemp | -20°C |
|---|---|
| ShipTemp | Ambient |
| InfoSheet | P3540InfoSheetPDF |
|---|
BuchananCM,DicksonJM,LeeWJ,etal.Oncogenicmutationsofp110αisoformofPI3-kinaseupregulateitsproteinkinaseactivity.PLoSOne.2013Aug1;8(8):e71337.PMID:23936502.
AoyagiK,Ohara-ImaizumiM,NishiwakiC,etal.AcuteinhibitionofPI3K-PDK1-Aktpathwaypotentiatesinsulinsecretionthroughupregulationofnewcomergranulefusionsinpancreaticβ-cells.PLoSOne.2012;7(10):e47381.PMID:23077605.
SmirnovaT,ZhouZN,FlinnRJ,etal.Phosphoinositide3-kinasesignalingiscriticalforErbB3-drivenbreastcancercellmotilityandmetastasis.Oncogene.2012Feb9;31(6):706-15.PMID:21725367.
DagiaNM,AgarwalG,KamathDV,etal.Apreferentialp110alpha/gammaPI3KinhibitorattenuatesexperimentalinflammationbysuppressingtheproductionofproinflammatorymediatorsinaNF-kappaB-dependentmanner.AmJPhysiolCellPhysiol.2010Apr;298(4):C929-41.PMID:20089935.
