GSK840-GSK-840-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGSK840Cat.No.:HY-104021CASNo.:2361146-30-5Synonyms:GSK'840分?式:C??H??N?O?分?量:365.43作?靶點(diǎn):RIPkinase作?通路:Apoptosis儲(chǔ)存?式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:110mg/mL(301.02mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.7365mL13.6825mL27.3650mL5mM0.5473mL2.7365mL5.4730mL10mM0.2737mL1.3683mL2.7365mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.75mg/mL(7.53mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.75mg/mL(7.53mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.75mg/mL(7.53mM);ClearsolutionBIOLOGICALACTIVITY?物活性GSK840(GSK'840)?種受體相互作?蛋?激酶3(RIP3或RIPK3)抑制劑，?親和?結(jié)合RIP3激酶結(jié)構(gòu)域，IC50值為0.9nM，并抑制激酶活性，IC50值為0.3nM[1]。IC50&TargetIC50:0.3nM(RIP3)[1]體外研究GSK840(GSK'840)(0.01-3μM;24hours)blocksTNF-inducednecroptosisinaconcentration-dependentmanner[1].GSK840bindsthekinasedomainandinhibitskinaseactivitywithhighspecificity,targetingabroaderrangeofpro-necroticstimulithancanbeachievedwithRIP1kinaseinhibitors[1].CellViabilityAssay[1]CellLine:HumanHT-29cells(TNF10ng/ml+zVAD-fmk20μM+SMAC007100nM)Concentration:0.01-3μMIncubationTime:24hoursResult:BlockedTNF-inducednecroptosisinaconcentration-dependentmanner.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?CellDeathDiscov.2022Feb26;8(1):88.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].MandalP,etal.RIP3inducesapoptosisindependentofpronecrotickinaseactivity.MolCell.2014Nov20;56(4):481-95.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.