Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEKKL-35Cat.No.:HY-101866CASNo.:865285-29-6分?式:C??H?ClFN?O?分?量:317.7作?靶點(diǎn):Bacterial作?通路:Anti-infection儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:6.25mg/mL(19.67mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.1476mL15.7381mL31.4762mL5mM0.6295mL3.1476mL6.2952mL10mM0.3148mL1.5738mL3.1476mL請根據(jù)產(chǎn)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(fù)凍融造成的產(chǎn)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(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。BIOLOGICALACTIVITY?物活性KKL-35反式標(biāo)記反應(yīng)抑制劑，IC50值為0.9μM。IC50&TargetIC50:0.9μM(trans-translationtaggingreaction)[1]體外研究KKL-35exhibitsbroad-spectrumantibioticactivity.KKL-35preventsgrowthofB.anthracisandM.smegmatis1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEwithminimuminhibitoryconcentration(MIC)valuesoflessthan6μM.KKL-35inhibittrans-translationatsomestepbeforeproteolysisoftaggedproteins.KKL-35inhibitstaggingofDHFR-ns.AlargeamountofuntaggedDHFRisproducedinreactionswiththehighestconcentrationsofKKL-35,indicatingthatKKL-35doesnotinhibittranslation.KKL-35preventsgrowthofWTS.flexneriwithaMICof6μM,andadditionofKKL-35toagrowingcultureofS.flexneristopsgrowth.InanS.flexneristrainexpressingArfAanddeletedforssrA,additionofKKL-35haslittleeffectonviabilityorgrowthrate.KKL-35inhibitsthegrowthofE.coli?tolC,whichisdeficientinsmallmoleculeefflux,withanMICof0.3μM[1].體內(nèi)研究EvidencesuggestthattheinvivoeffectsofKKL-35arecausedbyinhibitionofthereleaseofnonstoptranslationcomplexesbytrans-translation.KKL-35inhibitstrans-translationandpreventsgrowthofS.flexneristrainsthatrequiretrans-translation.Thecorrelationbetweeninhibitionoftrans-translationandgrowthissupportedbygeneticandpharmacologicalexperimentsshowingthatalternativemechanismstoreleasenonstoptranslationcomplexesrelievethegrowthsuppressionofKKL-35[1].REFERENCES[1].RamadossNS,etal.Smallmoleculeinhibitorsoftrans-translationhavebroad-spectrumantibioticactivity.ProcNatlAcadSciUSA.2013Jun18;110(25):10282-7.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearch