MKK7-COV-9-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMKK7-COV-9Cat.No.:HY-122872CASNo.:2283355-59-7分?式:C??H??N?O?分?量:320.35作?靶點(diǎn):p38MAPK作?通路:MAPK/ERKPathway儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:50mg/mL(156.08mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.1216mL15.6079mL31.2159mL5mM0.6243mL3.1216mL6.2432mL10mM0.3122mL1.5608mL3.1216mL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(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(7.80mM);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:≥2.5mg/mL(7.80mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.80mM);ClearsolutionBIOLOGICALACTIVITY?物活性MKK7-COV-9?種有效的、選擇性的MKK7共價(jià)抑制劑，靶向MKK7的?種特異性蛋?-蛋?相互作?。MKK7-COV-9阻斷了原代B細(xì)胞應(yīng)對(duì)LPS的激活的EC50值為4.98μM.IC50&Targetp38MAPkinase體外研究Duetopoorpermeability,thepiperidineanalogsMKK7-COV-10andMKK7-COV-11provestobeinactiveinICWin3T3cells,aswellasthecarboxylicacidMKK7-COV-8.Incontrast,asanamidecounterpart,MKK7-COV-9,retainsactivity(EC50=4.06μM)andfurthermorenowprovidesanewvectorforfurtherderivatization[1].MKK7-COV-9(10μM;48hours)showslimitedcytotoxiceffectonlyatthehighesttestedconcentration.Onlyonecellline,HCT116,displayedhalf-maximallethaldose(LD50)[1].MKK7-COV-9(10μM;2hrpre-incubation)isabletoinhibit60%oftheCD86+responseinresponsetoLPSstimulation,inprimarymouseBcells,exceptthenegativecontrolMKK7-NEG-1[1].JNKisknowntomediateactivationofBcellsinresponsetolipopolysaccharide(LPS;HY-D1056)throughtheTLR4signalingpathway.MKK7-COV-9(0-10μM;2hrpre-incubation)isabletomediateactivationofBcellsinresponsetoLPSthroughtheTLR4signalingpathway,itshowsadose-responsecurvesforinhibitionofLPSinducedactivationandexhibitsanEC50valueof4.98μM.(EC50=4.98μMforMKK7-COV-12;EC50>10μMforMKK7-COV-7;EC50=2.23μMforJNK-IN-8)[1].CellViabilityAssay[1]CellLine:MDAMB231,HCT116,HT29,COLO205,HELA,Z93T,PC3,4T1,A549,PC9,MDAMB468Concentration:0-10μMIncubationTime:48hoursResult:ShowedlittlecytotoxiceffectexceptforHCT116cells.REFERENCES[1].AmitShraga,etal.CovalentDockingIdentifiesaPotentandSelectiveMKK7Inhibitor.CellChemBiol.2019Jan17;26(1):98-108.e5.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical