KDM2A-7A-IN-1-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEKDM2A/7A-IN-1Cat.No.:HY-108706CASNo.:2169272-46-0分?式:C??H??N?O分?量:506.68作?靶點(diǎn):HistoneDemethylase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)DMSO:200mg/mL(394.73mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.9736mL9.8682mL19.7363mL5mM0.3947mL1.9736mL3.9473mL10mM0.1974mL0.9868mL1.9736mL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.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥5mg/mL(9.87mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥5mg/mL(9.87mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥5mg/mL(9.87mM);ClearsolutionBIOLOGICALACTIVITY?物活性KDM2A/7A-IN-1?種?創(chuàng)、選擇性、細(xì)胞通過性的組蛋?賴氨酸去甲化酶KDM2A/7A抑制劑，對(duì)KDM2A的IC50值為0.16μM，對(duì)其選擇性對(duì)其他JmjC賴氨酸去甲化酶的75倍，同時(shí)對(duì)甲轉(zhuǎn)移酶和組蛋??酰轉(zhuǎn)移酶?作?[1]。IC50&TargetIC50:0.16μM(KDM2A)[1]體外研究KDM2A/7A-IN-1((S,S)-6)isafirst-in-class,selectiveandcell-permeableinhibitorofhistonelysinedemethylasesKDM2A/7A,withanIC50of0.16μMforKDM2A,exhibits75foldselevtivityoverotherJmjClysinedemethylases,andisinactivetomethyltransferases,andhistoneacetyltransferases[1].KDM2A/7A-IN-1(0.4,3.1,6.2μM)augmentscellularH3K36me2levelsinHeLacellsectopicallyexpressingcatalyticallyactiveKDM2A[1].REFERENCES[1].GerkenPA,etal.DiscoveryofaHighlySelectiveCell-ActiveInhibitoroftheHistoneLysineDemethylasesKDM2/7.AngewChemIntEdEngl.2017Dec4;56(49):15555-15559.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:40