GSK621-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGSK621Cat.No.:HY-100548CASNo.:1346607-05-3分⼦式:C₂₆H₂₀ClN₃O₅分⼦量:489.91作⽤靶点:AMPK;Autophagy;Apoptosis作⽤通路:Epigenetics;PI3K/Akt/mTOR;Autophagy;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:12.5mg/mL(25.51mM;ultrasonicandadjustpHto1withHCl)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0412mL10.2060mL20.4119mL5mM0.4082mL2.0412mL4.0824mL10mM0.2041mL1.0206mL2.0412mL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:1.25mg/mL(2.55mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—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:≥1.25mg/mL(2.55mM);Suspendedsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥1.25mg/mL(2.55mM);Clearsolution4.请依序添加每种溶剂：50%PEG300>>50%salineSolubility:10mg/mL(20.41mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性GSK621特异性的AMPK激动剂，其对AML细胞系的IC50值为13-30μM。GSK621可诱导⾃噬和凋亡。GSK621可诱导eiF2α磷酸化(UPR激活的⼀个标志)。体外研究GSK621(30μM)inducesAMPKαT172,ACC(S79)andULK1(S555)phosphorylation[1].GSK621(30μM)inducesautophagyandapoptosis[1].GSK621treatmentalsoinducesPERKphosphorylation,amarkerofERstress,inAMLcells[1].CellProliferationAssay[1]CellLine:MV4-11,OCI-AML3,OCI-AML2,HL-60,Kasumi,HEL,UT7,NB4,TF-1,KG1A,Nomop28,SKM-1,U937,YHP1,MOLM-14,Mo7e,K562,MOLM-13,EOL-1,SET-2AMLcelllines.0-30μM.Concentration:0-30μM.IncubationTime:4d.Result:IC50valuesrangedfrom13to30μM.Reducedtheproliferationofall20linesandincreasedapoptosisin17(85%)lines.CellAutophagyAssay[1].CellLine:AMLcelllinesandprimaryAMLsamples.Concentration:30μM.IncubationTime:24h.Result:Inducedtheformationofnumerousintracytoplasmicvacuolesincludingautophagosomes.体内研究GSK621(30mg/kg,iptwicedaily)exhibitssignificantanti-tumoractivityinMOLM-14cellsxenograft[1].AnimalModel:MOLM-14cellsxenograftedintonudemice[1].Dosage:30mg/kg.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAdministration:IPtwicedaily.Result:Reducedleukemiagrowthandsignificantlyextendedsurvivalcomparedtovehicle-treatedanimalsorthosetreatedwith10mg/kgtwicedaily.户使⽤本产品发表的科研⽂献•EMBOJ.2021Sep2;e108028.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].PierreSujobert,etal.Co-activationofAMPKandmTORC1InducesCytotoxicityinAcuteMyeloidLeukemia.CellRep.2015Jun9;11(9):1446-57.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfor