KN-93isaninhibitorofcalmodulin-dependentkinaseII(CaMKII);itmayalsoinhibitL-typeCa2+channels.KN-93exhibitsanticancer,anti-arrhythmic,cardiomodulatory,antinociceptive,andimmunomodulatoryactivities.Invitro,KN-93decreasesVEGFexpression.WhencombinedwithVEGFinhibitors,thiscompounddecreasestumorgrowthinanimalmodelsofcancer.Inotheranimalmodels,KN-93preventsthedevelopmentofarrhythmiaandincreaseslevelsofTregcells.KN-93alsoincreaseswithdrawallatencyinanimalmodelsofthermalandmechanicalpain.
| CasNo. | 1188890-41-6 |
|---|---|
| Purity | ≥98% |
| Formula | C26H29ClN2O4S・H3O4P |
| FormulaWt. | 599.03 |
| IUPACName | N-[2-({[(2E)-3-(4-Chlorophenyl)-2-propen-1-yl](methyl)amino}methyl)phenyl]-N-(2-hydroxyethyl)-4-methoxybenzenesulfonamidephosphate(1:1) |
| Synonym | 2-[N-(2-Hydroxyethyl)-N-(4-methoxybenzenesulfonyl)]amino-N-(4-chlorocinnamyl)-N-methylbenzylamine |
| Solubility | Solubleinwater |
| Appearance | Whitetooff-whitesolid. |
| StoreTemp | 4°C |
|---|---|
| ShipTemp | Ambient |
| InfoSheet | K5200InfoSheetPDF |
|---|
TakeuchiM,YamamotoT.ApoptosisinducedbyNADdepletionisinhibitedbyKN-93inaCaMKII-independentmanner.ExpCellRes.2015Jul1;335(1):62-7.PMID:26024774.
TzimasC,TerrovitisJ,LehnartSE,etal.Calcium/calmodulin-dependentproteinkinaseII(CaMKII)inhibitionamelioratesarrhythmiaselicitedbyjunctinablationunderstressconditions.HeartRhythm.2015Jul;12(7):1599-610.PMID:25814413.
DaftPG,YangY,NapieralaD,etal.ThegrowthandaggressivebehaviorofhumanosteosarcomaisregulatedbyaCaMKII-controlledautocrineVEGFsignalingmechanism.PLoSOne.2015Apr10;10(4):e0121568.PMID:25860662.
BianH,YuLC.Intra-nucleusaccumbensadmiNISTrationofthecalcium/calmodulin-dependentproteinkinaseIIinhibitorKN93inducedantinociceptioninratswithmononeuropathy.NeurosciLett.2014Nov7;583:6-10.PMID:25218714.
KogaT,MizuiM,YoshidaN,etal.KN-93,aninhibitorofcalcium/calmodulin-dependentproteinkinaseIV,promotesgenerationandfunctionofFoxp3⁺regulatoryTcellsinMRL/lprmice.Autoimmunity.2014Nov;47(7):445-50.PMID:24829059.
