LCAHA-LCA-hydroxyamide-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELCAHACat.No.:HY-120458CASNo.:117094-40-3Synonyms:LCAhydroxyamide分⼦式:C₂₄H₄₁NO₃分⼦量:391.59作⽤靶点:Deubiquitinase作⽤通路:CellCycle/DNADamage储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:45mg/mL(114.92mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.5537mL12.7685mL25.5369mL5mM0.5107mL2.5537mL5.1074mL10mM0.2554mL1.2768mL2.5537mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(5.31mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.31mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性LCAHA(LCAhydroxyamide)⼀种脱泛素酶USP2a抑制剂，在Ub-AMC分析和Di-Ub分析中,IC50分别为9.7μM和3.7μM。LCAHA通过抑制去泛素酶USP2a破坏细胞周期蛋⽩D1稳定性并诱导G0/G1期阻滞[1]。体外研究LCAHAinhibitsHCT116wtandHCT116p53-/-coloncancercellsviabilitywithGI50sof0.87±0.09and0.96±0.29μM,respectively,andtheLD50sof27.8±3.9and26.5±0.1μM,respectively[1].CellViabilityAssay[1]CellLine:HCT116wtandHCT116p53-/-coloncancercellsConcentration:0.01,0.1,1,10,and100μMIncubationTime:6daysResult:TheGI50sare0.87±0.09and0.96±0.29μMforHCT116wtandHCT116p53-/-coloncancercells,respectively.REFERENCES[1].KatarzynaMagiera,etal.LithocholicAcidHydroxyamideDestabilizesCyclinD1andInducesG/G1ArrestbyInhibitingDeubiquitinaseUSP2a.CellChemBiol.2017Apr20;24(4):458-470.e18.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-82