SHIN1-RZ-2994-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESHIN1Cat.No.:HY-112066CASNo.:2146095-85-2Synonyms:RZ-2994分⼦式:C₂₄H₂₄N₄O₂分⼦量:400.47作⽤靶点:Others作⽤通路:Others储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:66.67mg/mL(166.48mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4971mL12.4853mL24.9707mL5mM0.4994mL2.4971mL4.9941mL10mM0.2497mL1.2485mL2.4971mL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%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥1.25mg/mL(3.12mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥1.25mg/mL(3.12mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥1.25mg/mL(3.12mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性SHIN1(RZ-2994)⼈丝氨酸羟甲转移酶1和2(SHMT1/2)抑制剂，体外实验中的其IC50值分别为5和13nM。IC50&TargetIC50:5nM(SHMT1),13nM(SHMT1)[1]体外研究SHIN1(RZ-2994)inhibitshumanSHIN1SHMT1/2withIC50sof5and13nM,respectivelyinaninvitroassay.SHIN1inhibitsthegrowthofSHMT2deletionHCT-116cellswithanIC50of10nM.SHIN1(RZ-2994)inhibitsSHMT1/2inHCT-116cells.SHIN1(RZ-2994)isparticularlyactiveagainstB-cellmalignancies.SHIN1blockscellgrowththroughaprogressivedepletionofpurines,leadingtolossofnucleotidetriphosphates[1].PROTOCOLCellAssay[1]Forproliferationassays,HCT-116cellsaretreatedwithSHIN1(1,10,100,1000,10000nM)for24-72hours.CellnumberwascounteddirectlyusingTrypanblueandtheCountesssystem[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•MolCell.2019Sep19;75(6):1147-1160.e5.•CommunBiol.2022Jun23;5(1):619.•CancerMetab.2020Sep21;8:20.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].DuckerGS,etal.HumanSHMTinhibitorsrevealdefectiveglycineimportasatargetablemetabolicvulnerabilityofdiffuselargeB-celllymphoma.ProcNatlAcadSciUSA.2017Oct24;114(43):11404-11409.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forre