CCT020312-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECCT020312Cat.No.:HY-119240CASNo.:324759-76-4分?式:C??H??Br?N?O?分?量:650.4作?靶點(diǎn):PERK;Autophagy作?通路:CellCycle/DNADamage;Autophagy儲存?式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(153.75mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.5375mL7.6876mL15.3752mL5mM0.3075mL1.5375mL3.0750mL10mM0.1538mL0.7688mL1.5375mL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(fù)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?jiān)?個?內(nèi)使?，-20°C儲存時，請?jiān)?個?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥?式選擇適當(dāng)?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(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(3.20mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:2.08mg/mL(3.20mM);Suspendedsolution;Needultrasonic3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.20mM);ClearsolutionBIOLOGICALACTIVITY?物活性CCT020312選擇性的EIF2AK3/PERK的激活劑。CCT020312可誘導(dǎo)細(xì)胞細(xì)胞中EIF2A的磷酸化。IC50&TargetEIF2AK3/PERK[1][2].體外研究TreatmentofHT29cellswithCCT020312for24hoursrevealsaconcentration-dependentlossofP-S608-pRBsignal,withalinearresponsebetween1.8and6.1μM[1].CCT020312treatmenteffectivelyinhibitscellproliferation(asmeasuredat96hours)eveniftreatmentisfor2hoursonlywithsubsequentcompoundwashout,indicatingthatCCT020312iscapableofelicitingdurableratherthantransientcytostasis[1].TreatmentofHT29cellswith10μMCCT020312for24hoursreducestheamountoftheG1/ScyclinsD1,D2,EandAaswellastheCDKcatalyticsubunitCDK2andincreasedtheleveloftheCDKinhibitorp27KIP1presentinsuchcells[1].體內(nèi)研究Treatmentof15-week-oldwildtypemicewiththePERKactivatorCCT020312(1-5mg/kg;i.p.;oncedailyfor3days)leadstoincreasedlevelsofphosphorylatedPERKandNRF2inbrainhomogenates[2].P301StransgenicmicetreatedwithCCT020312(2mg/kg;i.p.;oncedailyfor6weeks)performessignificantlybetterinMorriswatermaze[2].AnimalModel:9-week-oldP301Stautransgenicmice[2]Dosage:2mg/kgAdministration:Intraperitonealinjection;oncedailyfor6weeksResult:P301StransgenicmicetreatedwithCCT020312performedsignificantlybetterinMorriswatermaze.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?CellMetab.2021Mar2;33(3):598-614.e7.?CellDeathDis.2020Oct13;11(10):847.?OxidMedCellLongev.05Aug2022.?CellBiolToxicol.2022Jan14.?FrontCellDevBiol.04August2021.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[1].StockwellSR,etal.Mechanism-basedscreenforG1/ScheckpointactivatorsidentifiesaselectiveactivatorofEIF2AK3/PERKsignalling.PLoSOne.2012;7(1):e28568.[2].BruchJ,etal.PERKactivationmitigatestaupathologyinvitroandinvivo.EMBOMolMed.2017Mar;9(3):371-384.McePdfHeightCaution:Producthasnotbeenfullyvalid