.product-side h2 span {width: 50%;}.product-side h2 span.hover {}Related ProductsE-64Aprotinino-PhenanthrolineBestatinPepstatin AAEBSF.HClMolarity CalculatorDilution Calculator Leupeptin, MicrobialInhibitor of serine and cysteine proteasesCatalog No.A2570SizePriceStockQty25mg$100.00In stock Tel: +1-832-696-8203Email: sales@apexbt.comWorldwide Distributors Add to CartBulk InquiryFree samples Check OutSample solution is provided at 25 µL, 10mM.Publications citing ApexBio ProductsNature.2017 Jan 19;541(7637):417-420.Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Related Compound Libraries DiscoveryProbe™ Bioactive Compound LibraryDiscoveryProbe™ Protease Inhibitor LibraryQuality Control Quality Control & MSDS View current batch: 981 Purity = 98.00% COA (Certificate Of Analysis) MSDS (Material Safety Data Sheet) Datasheet Purity = 98.00% COA (Certificate Of Analysis) NMR (Nuclear Magnetic Resonance) MSDS (Material Safety Data Sheet) Datasheet Purity = 98.00% COA (Certificate Of Analysis) NMR (Nuclear Magnetic Resonance) MSDS (Material Safety Data Sheet) Datasheet Chemical structure Biological ActivityDescriptionLeupeptin, Microbial(Leupeptin hemisulfate ) is anreversible, competitive inhibitor of the proteases with Ki values of 0.13 nM and 7 nM for trypsin and cathepsin B, respectively.TargetsTrypsinCathepsin BIC500.13 nM (Ki)7 nM (Ki)ProtocolCell experiment [1]:Cell linesMRC-C cells infected with HCV 229EPreparation methodThe solubility of this compound in DMSO is ≥49.35mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.Reaction Conditions0, 1, 10 and 100 μg/mL; 24 hrsApplicationsIn cultures of MRC-C cells, Leupeptin prevented multiplication of the human coronavirus strain 229E. The IC50 value of Leupeptin in plaque tests was 0.4 μg/mL, whilst growth of host cells was unaffected by Leupeptin at 50 μg/mL. In single-cycle growth experiments, Leupeptin (100 μg/mL) reduced virus yield only if added within 2 hrs of infection, indicating its action on an early stage of virus replication.Animal experiment [2]:Animal modelsC57BL/6NCrl male miceDosage form0, 9, 18 36 and 40 mg/kg; i.p.ApplicationsLeupeptin was well tolerated by the animals and dose-dependently produced a substantial increase in LC3b-II in both the total tissue extracts and the lysosome enriched fraction (LE fraction). At the electron microscopy (EM) level, leupeptin induced the accumulation of electron-dense vesicular structures that, in hepatocytes, were visible by 60 min after treatment (40 mg/kg). The results suggested that Leupeptin enhanced LC3b-II levels in vivo by protecting this protein from being degraded inside lysosomes, and thus the leupeptin-based assay could be potentially used for studying the dynamics of macroautophagy in mice.Other notesPlease test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.References:[1]. Appleyard G, Tisdale M. Inhibition of the growth of human coronavirus 229E by leupeptin. Journal of general virology, 1985, 66(2): 363-366.[2]. Haspel J, Shaik RS, Ifedigbo E, Nakahira K, Dolinay T, Englert JA, Choi AM. Characterization of macroautophagic flux in vivo using a leupeptin-based assay. Autophagy. 2011 Jun;7(6):629-42.Leupeptin, Microbial Dilution CalculatorConcentration (start)xVolume (start)=Concentration (final)xVolume (final) femtomolar picomolar nanomolar micromolar millimolar molar nanoliter microliter milliliter liter femtomolar picomolar nanomolar micromolar millimolar molar microliter milliliter liter C1V1C2V2calculateLeupeptin, Microbial Molarity CalculatorMass=ConcentrationxVolumexMW* picograms nanograms micrograms milligrams grams kilograms femtomolar picomolar nanomolar micromolar millimolar molar nanoliter microliter milliliter liter g/molcalculate Chemical Properties Cas No. 103476-89-7SDF Download SDF Synonyms Leupeptin hemisulfate salt microbial,L-Leucinamide,Leupeptin, Microbial Chemical Name 2-acetamido-N-(1-((5-((diaminomethylene)amino)-1-oxopentan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)-4-methylpentanamide Canonical SMILES O=C(C(C([H])([H])C(C([H])([H])[H])([H])C([H])([H])[H])([H])N([H])C(C([H])([H])[H])=O)N([H])C(C(N([H])C(C([H])=O)([H])C([H])([H])C([H])([H])C([H])([H])/N=C(N([H])[H])/N([H])[H])=O)([H])C([H])([H])C(C([H])([H])[H])([H])C([H])([H])[H] Formula C20H38N6O4.1/2H2SO4 M.Wt 493.6 Solubility ≥24.7mg/mL in DMSO Storage Store at -20°CThe product is not stable in solution, please dissolve it immediately before use.Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon requestGeneral tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. BackgroundLeupeptin is a reversible inhibitor of protease with Ki values of 35 nM, 3.4 μM, 6 nM and 72 nM for bovine trypsin, human plasmin, bovine spleen cathepsin B and recombinant human calpain, respectively [1, 2].As a protease inhibitor, leupeptin was originally isolated from the Streptomyces species. It exerted poor membrane permeability due to its polar C-terminal. For calpain, leupeptin showed moderate potent activities with IC50 values of 0.211 μM, 1.8 μM and 0.938 μM against the enzymes isolated from porcine erythrocyte, porcine kidney and human platelet, respectively. In cultured MRC-C cells, leupeptin suppressed the growth of human coronavirus strain 229E through inhibited the activity of trypsin. The mean IC50 value was 0.8 μM [2, 3].References: 1.  Mehdi S. Cell-penetrating inhibitors of calpain. Trends in biochemical sciences, 1991, 16: 150-153. 2.  Krauser J A, Powers J C. 6.1 BIOLOGICAL ROLES. Proteinase and Peptidase Inhibition: Recent Potential Targets for Drug Development, 2003: 144. 3.  Appleyard G, Tisdale M. Inhibition of the growth of human coronavirus 229E by leupeptin. Journal of general virology, 1985, 66(2): 363-366.