Name: CA-074 Me
Price: 268.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    CA-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].
    
    [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.
- Properties
  - Alternative Name
    
    methyl (2S)-1-[(2S)-3-methyl-2-[[(2S,3S)-3-(propylcarbamoyl)oxirane-2-carbonyl]amino]pentanoyl]pyrrolidine-2-carboxylate
    
    CAS Number
    
    147859-80-1
    
    Molecular Formula
    
    C19H31N3O6
    
    Molecular Weight
    
    397.5
    
    Appearance
    
    A solid
    
    Purity
    
    96.29%
    
    Solubility
    
    insoluble in H2O; ≥19.88 mg/mL in DMSO; ≥51.5 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Jianhua Wang, Lichun Wang, et al. "Cathepsin B aggravates acute pancreatitis by activating the NLRP3 inflammasome and promoting the caspase-1-induced pyroptosis." Int Immunopharmacol. 2021 May;94:107496. PMID:33639565
    2. Zhi X, Zhang Y, et al. "NLRP3 inflammasome activation by Foot-and-mouth disease virus infection mainly induced by viral RNA and non-structural protein 2B." RNA Biol. 2020;17(3):335–349. PMID:31840571
    3. Zhou H, Du R, et al. "Cannabinoid receptor 2 promotes the intracellular degradation of HMGB1 via the autophagy-lysosome pathway in macrophage." Int Immunopharmacol. 2020;78:106007. PMID:31806570
    4. Chen CH, Bhasin S, et al. "Study of Cathepsin B inhibition in VEGFR TKI treated human renal cell carcinoma xenografts." Oncogenesis. 2019 Feb 22;8(3):15. PMID:30796200
    5. Xu Z, Zhang Y, et al. "Novel half-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:30673591
    6. 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:30578561
    7. Gonzalez EA, Martins GR, et al. "Cathepsin B inhibition attenuates cardiovascular pathology in mucopolysaccharidosis I mice." Life Sci. 2018 Mar 1;196:102-109. PMID:29366749
    8. 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:29455656
    9. 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:29203413

CA-074 Me

CA-074 Me

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