MS049-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMS049Cat.No.:HY-100360CASNo.:1502816-23-0分?式:C??H??N?O分?量:248.36作?靶點(diǎn):HistoneMethyltransferase作?通路:Epigenetics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)H2O:≥100mg/mL(402.64mM)DMSO:≥31mg/mL(124.82mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM4.0264mL20.1321mL40.2641mL5mM0.8053mL4.0264mL8.0528mL10mM0.4026mL2.0132mL4.0264mL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)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(10.07mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(10.07mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(10.07mM);Clearsolution4.請(qǐng)依序添加每種溶劑：PBSSolubility:100mg/mL(402.64mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性MS049?種?效、選擇性和細(xì)胞活性的PRMT4和PRMT6雙重抑制劑，IC50分別為34nM和43nM。MS049降低了HEK293細(xì)胞的Med12me2a和H3R2me2a?平。MS049對(duì)HEK293細(xì)胞?毒，并且沒有響其的?長(zhǎng)[1]。IC50&TargetPRMT4PRMT6PRMT834nM43nM1600nM體外研究MS049(0.1-10μM;20hours)reducestheH3R2me2amarkinHEK293cellsinaconcentrationdependentmanner(IC50=0.97±0.05μM)[1].MS049(0.1-100μM;72hours)inhibitsendogenousPRMT4methyltransferaseactivityinaconcentrationdependentmannerresultinginreducedlevelsofcellularasymmetricargininedimethylationofMed12(Med12-Rme2a,IC50=1.4±0.1μM)inHEK293cells[1].MS049isselectiveforPRMT4andPRMT6overabroadrangeofepigeneticmodifiers,includingotherPRMTs,PKMTs,DNMTs,KDMs,andmethyllysine/methylargininereaderproteins,andnon-epigenetictargets[1].WesternBlotAnalysis[1]CellLine:HEK293cellsConcentration:0.1,1,10μMIncubationTime:20hoursResult:ReducedtheH3R2me2amarkinHEK293cellsinaconcentrationdependentmanner(IC50=0.97±0.05μM).WesternBlotAnalysis[1]CellLine:HEK293cellsConcentration:0.1,1,10,100μMIncubationTime:72hours2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEResult:ReducedlevelsofcellularasymmetricargininedimethylationofMed12(Med12-Rme2a,IC50=1.4±0.1μM)inHEK293cells.REFERENCES[1].ShenYetal.DiscoveryofaPotent,Selective,andCell-ActiveDualInhibitorofProteinArginineMethyltransferase4andProteinArginineMethyltransferase6.JMedChem.2016Sep15.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical