GSK963-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGSK963Cat.No.:HY-103028ACASNo.:2049868-46-2分?式:C??H??N?O分?量:230.31作?靶點:RIPkinase作?通路:Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:25mg/mL(108.55mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM4.3420mL21.7099mL43.4197mL5mM0.8684mL4.3420mL8.6839mL10mM0.4342mL2.1710mL4.3420mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(10.85mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(10.85mM);ClearsolutionBIOLOGICALACTIVITY?物活性GSK963?種?性的、強效的、選擇性的受體相互作?蛋?1(RIP1)酶的抑制劑，其IC50值為29nM。GSK963對體外??和?細胞的壞死具有強效和選擇性的抑制作?。IC50&TargetIC50:29nM(RIP1inFPbindingassay)[1].體外研究GSK963is>10?000-foldselectiveforRIP1over339otherkinases,lacksmeasurableactivityagainstIDOandhasaninactiveenantiomer,GSK962,whichcanbeusedtoconfirmon-targeteffects[1].體內研究GSK963(2mg/kg)resultsinacompleteprotectionfromTNF+zVAD-inducedtemperatureloss.GSK963(0.2?mg/kg)alsoshowsasignificantresponse[1].AnimalModel:C57BL/6mice[1].Dosage:0.2mg/kg,2mg/kg,10?mg/kg.Administration:IPonce.Result:ProtectedmicefromTNF+zVAD-inducedhypothermia.REFERENCES[1].BergerSB,etal.CharacterizationofGSK'963:astructurallydistinct,potentandselectiveinhibitorofRIP1kinase.CellDeathDiscov.2015Jul27;1:15009.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-8