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SD169isanindole-5-carboxamide,orally-available,ATP-competitive,a-selectivep38MAPKinhibitorthattargetsawidevarietyofinflammatorycells,includingneutrophils,monocytes,macrophages,BandCD4+Tcells,andendothelialcells.[1]ThroughinteractionswithSchwanncellandTNFactivity,SD169promotesaxonalregenerationinperipheralnerves.[2]
SD169hasbeenshowntoreducemyeloma-inducedosteolyticbonelesionsandrestoredbonemassbydownregulatingosteoclastogenesisandosteoblastogenesisinxenograftedprimarymyeloma-SCID-huormyelomacellline-SCIDmousemodels.[3]SD169wasalsoshowndownregulatespp38inmyelomacellsinvitroandinvivo.
Inthediabetestherapeuticarea,SD169significantlyreducesp38andHSP60expressioninTcellsofthepancreaticbetaislets.InstudiesusinghyperglycemicNODmice,SD169treatmentloweredbloodglucoseandimprovedglucosehomeostasis.[4]
Technicalinformation:
| ChemicalFormula: | C9H8N2O | |
| CAS#: | 1670-87-7 | |
| MolecularWeight: | 160.17 | |
| Purity: | >98% | |
| Appearance: | White | |
| ChemicalName: | 1H-indole-5-carboxamide | |
| Solubility: | Upto22mMinDMSO | |
| Synonyms: | SD-169,SD169 |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | Medicherlaetal.,p38MAPKinhibitionreducesdiabetes-inducedimpairmentofwoundhealing.Diabetes,Metab.Syndr.Obes.2009,2,91-100.PubmedID:21437122 |
| 2. | Myersetal.,Inhibitionofp38MAPkinaseactivityenhancesaxonalregeneration.Exp.Neurol.2003,184,606-614.PubmedID:14769353 |
| 3. | Yangetal.,Constitutiveactivationofp38MAPKintumorcellscontributestoosteolyticbonelesionsinmultiplemyeloma.Leukemia,2012,26,2114-2123.PubmedID:22425892 |
| 4. | Medicherlaetal.,J.Pharmacol.Exp.Ther.2006,318(1),99-107.PubmedID:14769353 |