DCH36-06-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEDCH36_06Cat.No.:HY-139108CASNo.:593273-05-3分?式:C??H??ClN?O?S分?量:372.83作?靶點(diǎn):HistoneAcetyltransferase;Apoptosis作?通路:Epigenetics;Apoptosis儲(chǔ)存?式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:125mg/mL(335.27mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.6822mL13.4109mL26.8219mL5mM0.5364mL2.6822mL5.3644mL10mM0.2682mL1.3411mL2.6822mL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(protectfromlight)。-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:≥2.08mg/mL(5.58mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(5.58mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性DCH36_06?種有效的選擇性p300/CBP抑制劑，對(duì)p300和CBP的IC50分別為0.6μM和3.2μM。DCH36_06介導(dǎo)的p300/CBP抑制導(dǎo)致??病細(xì)胞中H3K18的低?酰化?？鼓[瘤活性。體外研究DCH36_06(6.7-20μM;24-48hours)treatmentarrestscellcycleatG1phaseandinducesapotosisinadose-dependentmannerinleukemiccells[1].DCH36_06(5-10μM;24hours)treatmentsignificantlyactivatesthecleavageofpro-caspase3,pro-caspase9andPARP1atdose-dependentmanner[1].DCH36_06showspotentantiproliferativeactivityagainsttestedleukemiacelllines(CEM,MOLT3,MOLT4,Jurkat,MV4-11,THP-1,RS4;11,KOPN8,Kasumi-1andK562cells)inadose-dependentmannerwithIC50valuesatsingle-digitmicromolarrange[1].CellCycleAnalysis[1]CellLine:MV4-11cellsConcentration:6.7μM,20μMIncubationTime:24hours,48hoursResult:Dose-dependentlyarrestedcellcycleatG1phase.ApoptosisAnalysis[1]CellLine:MV4-11cellsConcentration:6.7μM,20μMIncubationTime:24hours,48hoursResult:Significantlyinducedapoptosis.WesternBlotAnalysis[1]CellLine:MV4-11cellsConcentration:5μM,10μMIncubationTime:24hoursResult:Significantlyactivatedthecleavageofpro-caspase3,pro-caspase9andPARP1atdose-dependentmanner.體內(nèi)研究DCH36_06(25-50mg/kg;intraperitonealinjection;everytwodays;for20days)blockstheleukemicxenograftgrowthinmice[1].2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEAnimalModel:MV4-11xenograftnudemice[1]Dosage:25mg/kg,50mg/kgAdministration:Intraperitonealinjection;everytwodays;for20daysResult:Thetumorgrowthrateshowedsignificantreductionindose-dependentmanner.REFERENCES[1].WenchaoLu,etal.Discoveryandbiologicalevaluationofthiobarbituricderivativesaspotentp300/CBPinhibitors.BioorgMedChem.2018Nov1;26(20):5397-5407.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfor