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

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECorinCat.No.:HY-111048CASNo.:1808113-09-8分?式:C??H??N?O?分?量:428.53作?靶點(diǎn):HistoneDemethylase;HDAC作?通路:Epigenetics;CellCycle/DNADamage儲(chǔ)存?式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(233.36mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.3336mL11.6678mL23.3356mL5mM0.4667mL2.3336mL4.6671mL10mM0.2334mL1.1668mL2.3336mL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(storedundernitrogen)。-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:≥2.5mg/mL(5.83mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.83mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性Corin組氨酸賴氨酸特異性去甲化酶(LSD1)和組氨酸脫??；?HDAC)的雙重抑制劑，其對(duì)LSD1的Ki(inact)值為110nM，對(duì)HDAC1的IC50值為147nM。IC50&TargetIC50:147nM(HDAC1),Ki(inact):110nM(LSD1)[1].體外研究Corinisabletoinhibitthedeacetylationofsemisynthetic,reconstitutednucleosomesbytheCoRESTternarycomplex.CorinshowsirreversibleinhibitionofHDAC1activity.InComparisontoMS-275,corinappearstomorepotently(CorinEC5095nMvs.MS-275EC50420nM)andefficaciouslyinducecellularH3K9acetylation.Interestingly,Corin(1μM)isnon-toxictoprimaryhumanmelanocytesincontrasttoMS-275(1μM)[1].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?NatStructMolBiol.2022Nov7.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].KalinJH,etal.TargetingtheCoRESTcomplexwithdualhistonedeacetylaseanddemethylaseinhibitors.NatCommun.2018Jan4;9(1):53.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel: