SRPIN340-SRPK-inhibitor-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESRPIN340Cat.No.:HY-13949CASNo.:218156-96-8Synonyms:SRPKinhibitor分⼦式:C₁₈H₁₈F₃N₃O分⼦量:349.35作⽤靶点:SRPK;VirusProtease作⽤通路:CellCycle/DNADamage;Anti-infection储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥42mg/mL(120.22mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.8625mL14.3123mL28.6246mL5mM0.5725mL2.8625mL5.7249mL10mM0.2862mL1.4312mL2.8625mL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)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(7.16mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性SRPIN340⼀种ATP竞争性的SRPK抑制剂，能够抑制SRPK1的活性，Ki值为0.89μM。IC50&TargetKi:0.89μM(SRPK1)[1]体外研究SRPIN340isaserine-arginine-richproteinkinase(SRPK)inhibitor,withaKiof0.89μMforSRPK1.SRPIN340alsoinhibitsSRPK2,butshowsnosignificantinhibitiononotherSRPK,suchasClk1andClk4.SRPIN340promotesdegradationofSRp75,whichisnecessaryforHIVexpression.SRPIN340suppressesthepropagationofSindbisvirus(IC50,60μM)aswellassevereacuterespiratorysyndromevirus[1].SRPIN340showsinhibitoryeffectonleukemiacelllines,suchasAMLHL60,ALL-TMolt4andJurkat,withIC50sof44.7μM,92.2μMand82.3μM,respectively[2].PROTOCOLCellAssay[2]Leukemiccells(5×104cells/well)andisolatedPBMCs(8×104cells/well)areseededin96-wellplates.Eachwellcontained100μLofcompleteRPMImediumand100μLofSRPIN340solutionatdifferentconcentrations.ThecompoundisdilutedinRPMImediumwith10%fetalbovineserumand0.4%DMSO(v/v).After48hofculture,MTT(5mg/mL)isaddedtothewells(3h,37°C).Theplatesarecentrifugedatroomtemperaturefor30min500×g,followedbytheremovaloftheMTTsolutionandtheadditionof100μL/wellofDMSOtosolubilizetheformazan.Absorbanceismeasuredat540nminamicroplatereader.Eachexperimentalprocedureisperformedintriplicate[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•NucleicAcidsRes.2021Mar18;49(5):2509-2521.•SciSignal.2022Oct25;15(757):eabm0808.•CellMolLifeSci.2022Aug5;79(8):467.•BMCCancer.2022Oct27;22(1):1100.•BiochemBiophysResCommun.2019Feb26;510(1):97-103.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].FukuharaT,etal.UtilizationofhostSRproteinkinasesandRNA-splicingmachineryduringviralreplication.ProcNatlAcadSciUSA.2006Jul25;103(30):11329-33.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[2].SiqueiraRP,etal.PotentialAntileukemiaEffectandStructuralAnalysesofSRPKInhibitionbyN-(2-(Piperidin-1-yl)-5-(Trifluoromethyl)Phenyl)Isonicotinamide(SRPIN340).PLoSOne.2015Aug5;10(8):e0134882.McePdfHeightCaution:Producthasnotbeenfully