POMHEX-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPOMHEXCat.No.:HY-131904CASNo.:2004714-34-3分⼦式:C₁₇H₃₀NO₉P分⼦量:423.4作⽤靶点:Enolase;Apoptosis作⽤通路:MetabolicEnzyme/Protease;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(236.18mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.3618mL11.8092mL23.6183mL5mM0.4724mL2.3618mL4.7237mL10mM0.2362mL1.1809mL2.3618mL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>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(5.90mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.90mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.90mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性POMHEX⼀个消旋混合物，具有细胞渗透性的HEX的POM前体药物，ENO2的特异性抑制剂。POMHEX对ENO1缺失的细胞表现出低纳尔级别活性，并对ENO1缺失的肿瘤模型表现出良好的抗癌效果。POMHEX有效的糖酵解抑制剂。体外研究POMHEX(78nM,8h)minimallyimpactsENO1-WTgliomacellsbutprofoundlyaffectedENO1-deletedcells[1].POMHEX(0-720nM)selectivelyinducesenergystress,inhibitsproliferationandtriggersapoptosisinENO1-deletedgliomacells[1].CellProliferationAssay[1]CellLine:ENO1-deleted(D423,red),ENO1-isogenicallyrescued(D423ENO1,blue)andENO1-WT(LN319,grey)cells.Concentration:78nM.IncubationTime:8h.Result:Down-regulatedcelldensity.体内研究POMHEX(i.v.,ip)injectionsareconsistentlytoleratedwithouthaemolyticanaemiaatdosesofupto10mgperkg(bodyweight)perday.POMHEX(i.v.,35mg/kg)resultsinlethargythatpromptedveterinarianstoperformeuthanasia[1].POMHEXisrapidlyhydrolysedtoHemiPOMHEXinmouseplasmaexvivo,withahalf-lifeofapproximately30s,thehalf-lifeinhumanbloodexvivowasabout9min[1].REFERENCES[1].Yu-HsiLin,etal.AnenolaseinhibitorforthetargetedtreatmentofENO1-deletedcancers.NatMetab.2020Nov23.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearc