.product-side h2 span {width: 50%;}.product-side h2 span.hover {}Related ProductsE-64-cCathepsin G Inhibitor ICA 074L 006235E 64dE-64Molarity CalculatorDilution Calculator CA-074 MeCathepsin B inhibitorCatalog No.A8239SizePriceStockQty10mM (in 1mL DMSO)$290.00In stock 1mg$85.00In stock 5mg$225.00In stock 10mg$375.00In stock 25mg$600.00In stock Tel: +1-832-696-8203Email: sales@apexbt.comWorldwide Distributors Add to CartBulk InquiryFree samples Check OutSample solution is provided at 25 µL, 10mM.Product Citations1. Chen CH, Bhasin S, et al. "Study of Cathepsin B inhibition in VEGFR TKI treated human renal cell carcinomaxenografts." Oncogenesis. 2019 Feb 22;8(3):15.PMID:307962002. Xu Z, Zhang Y, et al. "Novelhalf-sandwich iridium OˆC (carbene)-Complexes: In vitro and in vivo tumor growth suppression and pro-apoptosis via ROS-mediated cross-talk between mitochondria and lysosomes." Cancer Lett. 2019 Apr 10;447:75-85.PMID:306735913. Yan X, Li F, et al. "Interleukin-1beta released by microglia initiates the enhanced glutamatergic activity in the spinal dorsal horn during paclitaxel-associated acute pain syndrome." Glia. 2018 Dec 21.PMID:305785614. Gonzalez EA, Martins GR, et al. "Cathepsin B inhibition attenuates cardiovascular pathology inmucopolysaccharidosis I mice." Life Sci. 2018 Mar 1;196:102-109.PMID:293667495. Shao G, Wang R, et al. "The E3 ubiquitin ligase NEDD4 mediates cell migration signaling of EGFR in lung cancer cells." Mol Cancer. 2018 Feb 19;17(1):24.PMID:294556566. Clerc P, Jeanjean P, et al. "Targeted Magnetic Intra-Lysosomal Hyperthermia produces lysosomal reactive oxygen species and causes Caspase-1 dependent cell death." J Control Release. 2017 Dec 1;270:120-134.PMID:29203413Hide ↑↑Related Compound Libraries DiscoveryProbe™ Bioactive Compound LibraryDiscoveryProbe™ Protease Inhibitor LibraryQuality ControlQuality Control & MSDS View current batch:131298654321 Purity = 96.29% COA (Certificate Of Analysis) HPLC MS (Mass Spectrometry) MSDS (Material Safety Data Sheet) Datasheet Purity = 97.04% COA (Certificate Of Analysis) HPLC MS (Mass Spectrometry) NMR (Nuclear Magnetic Resonance) MSDS (Material Safety Data Sheet) Datasheet Purity = 97.34% COA (Certificate Of Analysis) HPLC NMR (Nuclear Magnetic Resonance) MSDS (Material Safety Data Sheet) Datasheet Purity = 98.49% COA (Certificate Of Analysis) HPLC NMR (Nuclear Magnetic Resonance) MSDS (Material Safety Data Sheet) Datasheet Purity = 98.44% COA (Certificate Of Analysis) HPLC NMR (Nuclear Magnetic Resonance) MSDS (Material Safety Data Sheet) Datasheet Purity = 98.01% COA (Certificate Of Analysis) HPLC NMR (Nuclear Magnetic Resonance) MSDS (Material Safety Data Sheet) Datasheet Purity = 98.64% COA (Certificate Of Analysis) HPLC (Retest) NMR (Nuclear Magnetic Resonance) MSDS (Material Safety Data Sheet) Datasheet Purity = 99.16% COA (Certificate Of Analysis) HPLC (Retest) NMR (Retest) MSDS (Material Safety Data Sheet) Datasheet Purity = 98.18% COA (Certificate Of Analysis) HPLC NMR (Nuclear Magnetic Resonance) MSDS (Material Safety Data Sheet) Datasheet Purity = 98.06% COA (Certificate Of Analysis) HPLC NMR (Nuclear Magnetic Resonance) MSDS (Material Safety Data Sheet) Datasheet Chemical structure Related Biological Data Related Biological Data Related Biological Data Related Biological Data Related Biological Data Related Biological Data Related Biological Data Biological ActivityDescriptionCA-074 Me is a selective and cell-permeable inhibitor of cathepsin B.Targetscathepsin BIC502.2 nMProtocolCell experiment: [1]Cell linesMcNtcp.24 cellsPreparation methodThe solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.Reaction Conditions0.1 µM, 2 hoursApplicationsCells were incubated in medium alone or with 50 µM GCDC in the absence or presence of 0.1 µM CA-074 Me. Apoptosis was quantitated after 2 h of incubation. The cathepsin B inhibitor CA-074 Me reduced the GCDC-mediated increase in cathepsin B activity and apoptosis in McNtcp.24 cells. The result confirms that cathepsin B activity increases and contributes to bile salt–mediated apoptosis in primary rat hepatocytes.Animal experiment: [2]Animal modelsCatB+/+ miceDosage formIntraperitoneal injection, 4 mg/100gApplicationsSerum ALT levels after TNF-α-treatment were significantly reduced in catB+/+ mice pretreated with CA-074 Me compared to saline-injected controls. In contrast, liver architecture was preserved and only moderate damage was observed in catB+/+ mice pretreated with CA-074 Me. These results suggest that pharmacological inhibition of cat B may partially attenuate TNF-α-induced liver damage.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] Faubion W A, Guicciardi M E, Miyoshi H, et al. Toxic bile salts induce rodent hepatocyte apoptosis via direct activation of Fas. The Journal of clinical investigation, 1999, 103(1): 137-145.[2] Guicciardi M E, Miyoshi H, Bronk S F, et al. Cathepsin B knockout mice are resistant to tumor necrosis factor-α-mediated hepatocyte apoptosis and liver injury: implications for therapeutic applications. The American journal of pathology, 2001, 159(6): 2045-2054.CA-074 Me 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 C1V1C2V2calculateCA-074 Me 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. 147859-80-1SDF Download SDF Synonyms N/A Chemical Name methyl (2S)-1-[(2S)-3-methyl-2-[[(2S,3S)-3-(propylcarbamoyl)oxirane-2-carbonyl]amino]pentanoyl]pyrrolidine-2-carboxylate Canonical SMILES CCCNC(=O)C1C(O1)C(=O)NC(C(C)CC)C(=O)N2CCCC2C(=O)OC Formula C19H31N3O6 M.Wt 397.5 Solubility ≥19.875mg/mL in DMSO Storage Store at -20°CPhysical AppearanceA yellow oilShipping 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. BackgroundCA-074 Me is a membrane-permeable and selective inhibitor of cathepsin B with IC50 value of 36.3 nM [1, 2].CA-074 Me is a methyl ester derivative of CA-074. In cultured human gingival fibroblasts, CA-074 Me exerted a 95% inhibition of cathepsin B and partial inhibition (54%) of the combined activities of cathepsins B and L. CA-074 Me was also found to inhibit cathespin L under reducing conditions. It inhibited the activity of purified human cathepsin L by more than 90% when the enzyme had been pre-incubated with 1.4 mM DTT or 4.2 mM GSH for 2 hours. Besides that, CA-074 Me completely inhibited cathepsin B in the presence of 1.4 mM DTT [2, 3].References:[1] Wu X, Zhang L, Gurley E, et al. Prevention of free fatty acid–induced hepatic lipotoxicity by 18β-glycyrrhetinic acid through lysosomal and mitochondrial pathways. Hepatology, 2008, 47(6): 1905-1915.[2] Steverding D. The cathepsin B-selective inhibitors CA-074 and CA-074Me inactivate cathepsin L under reducing conditions. Open Enzyme Inhibition Journal, 2011, 4: 11-16.[3] Buttle D J, Murata M, Knight C G, et al. CA074 methyl ester: a proinhibitor for intracellular cathepsin B. Archives of biochemistry and biophysics, 1992, 299(2): 377-380.