MKK7-COV-9-DataSheet-生命科學試劑-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:p38MAPK作?通路:MAPK/ERKPathway儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:50mg/mL(156.08mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.1216mL15.6079mL31.2159mL5mM0.6243mL3.1216mL6.2432mL10mM0.3122mL1.5608mL3.1216mL請根據產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?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?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儲存條件，適當保存；體內實驗的?作液，建議您現?現配，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沉淀、析出現象，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>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(7.80mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(7.80mM);Clearsolution3.請依序添加每種溶劑：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細胞應對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