SHIN1-RZ-2994-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESHIN1Cat.No.:HY-112066CASNo.:2146095-85-2Synonyms:RZ-2994分?式:C??H??N?O?分?量:400.47作?靶點:Others作?通路:Others儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:66.67mg/mL(166.48mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.4971mL12.4853mL24.9707mL5mM0.4994mL2.4971mL4.9941mL10mM0.2497mL1.2485mL2.4971mL請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥1.25mg/mL(3.12mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥1.25mg/mL(3.12mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥1.25mg/mL(3.12mM);ClearsolutionBIOLOGICALACTIVITY?物活性SHIN1(RZ-2994)?絲氨酸羥甲轉移酶1和2(SHMT1/2)抑制劑，體外實驗中的其IC50值分別為5和13nM。IC50&TargetIC50:5nM(SHMT1),13nM(SHMT1)[1]體外研究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.戶使?本產品發(fā)表的科研?獻?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