KB02-SLF-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEKB02-SLFCat.No.:HY-129610CASNo.:2384184-40-9分?式:C??H??ClN?O??分?量:949.52作?靶點(diǎn):PROTACs;FKBP作?通路:PROTAC;Apoptosis;Autophagy;Immunology/Inflammation儲(chǔ)存?式:4°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(105.32mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.0532mL5.2658mL10.5316mL5mM0.2106mL1.0532mL2.1063mL10mM0.1053mL0.5266mL1.0532mL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(sealedstorage,awayfrommoistureandlight)。-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(5.27mM);Suspendedsolution;Needultrasonic2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:5mg/mL(5.27mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥5mg/mL(5.27mM);ClearsolutionBIOLOGICALACTIVITY?物活性KB02-SLF?種于PROTAC的核FKBP12降解劑(molecularglue)。KB02-SLF通過共價(jià)修飾DCAF16(E3ligase)促進(jìn)FKBP12降解，并可以提??物系統(tǒng)中蛋?質(zhì)降解的持久性。KB02-SLF由SLF與泛素E3連接酶配體(KB02)通過linker連接?成。IC50&TargetFKBP12[1]體外研究KB02-SLF(2μM;4-72hours;HEK293Tcells)treatmentpromotesasubstantialreductioninnuclearFKBP12thatissustainedacrossa4-72htimeframe[1].Cellimagingstudiesconfirmstheselectivelossofnuclear-localizedFKBP12inKB02-SLF-treatedcells.KB02-SLFpromotesthelossofFKBP12_NLSacrossaconcentrationof~0.5-5μM,butshowsvariedreductionsinactivityathigherconcentrations.ThedegradationofFKBP12_NLSinducedbyKB02-SLFismediatedbyDCAF16[1].WesternBlotAnalysis[1]CellLine:HEK293TcellsConcentration:2μMIncubationTime:4hours,8hours,24hours,48hours,72hoursResult:PromotedasubstantialreductioninnuclearFKBP12thatwassustainedacrossa4-72htimeframe.REFERENCES[1].ZhangX,etal.ElectrophilicPROTACsthatdegradenuclearproteinsbyengagingDCAF16.NatChemBiol.2019Jul;15(7):737-746.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forre