CA-074
Based on 30 publication(s) in Google Scholar
CA-074 is a potent inhibitor of cathepsin B with a Ki of 2 to 5 nM.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 134448-10-5
- Formula: C18H29N3O6
- Molecular Weight:383.44
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
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Publications Citing Use of MedChemExpress (MCE) CA-074
More- Signal Transduct Target Ther. 2025 Dec 15;10(1):406. [Abstract]
- Cell. 2026 Feb 5;189(3):818-831.e19. [Abstract]
- Nat Mater. 2023 Nov;22(11):1421-1429. [Abstract]
- Nat Commun. 2020 Mar 27;11(1):1620. [Abstract]
- Autophagy. 2025 Mar 28. [Abstract]
- Adv Sci (Weinh). 2025 Dec 2:e04665. [Abstract]
- Adv Sci (Weinh). 2025 Aug 7:e09208. [Abstract]
- Biomaterials. 2022 Dec:291:121887. [Abstract]
- Genes Dis. 2025 Aug 14.
- Neoplasia. 2018 Oct;20(10):1008-1022. [Abstract]
- Emerg Microbes Infect. 2023 Dec;12(1):2207688. [Abstract]
- Mol Cell Proteomics. 2024 Jun;23(6):100775. [Abstract]
- J Enzyme Inhib Med Chem. 2024 Dec;39(1):2387417. [Abstract]
- PLoS Pathog. 2024 Feb 14;20(2):e1011981. [Abstract]
- Int J Mol Sci. 2022 Jul 7;23(14):7544. [Abstract]
- Int Immunopharmacol. 2024 Dec 9:145:113781. [Abstract]
- Sci Rep. 2022 Jul 16;12(1):12197. [Abstract]
- Environ Toxicol. 2021 Apr;36(4):520-529. [Abstract]
- Environ Toxicol. 2021 Feb;36(2):257-266. [Abstract]
- Xenobiotica. 2024 May 13:1-13. [Abstract]
- Res Sq. 2026 Feb 2.
- Res Sq. 2025 Dec 21.
- Maastricht University. 2025.
- Research Square Print. 2025 May 28.
- bioRxiv. 2025 May 05.
- bioRxiv. 2025 January 19.
- bioRxiv. 2023 Dec 14.
- bioRxiv. 2023 Nov 5.
- Research Square Print. December 8th, 2022.
- Research Square Preprint. 2021 Aug.
Customer Validation & Images
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Cell Proliferation/Viability Assay
All Cathepsin Isoforms
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Biological Activity
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Cathepsin B |
CA-074 is a synthetic analogue of E-64, a natural peptidyl epoxide that irreversibly inhibits most known lysosomal cysteine proteinases, and is developed by means of rational drug design, exploiting the dipeptidylcarboxypeptidase activity of cathepsin B. CA-074 can be used to selectively inhibit cathepsin B within living cells, as long as the experimental conditions permit significant fluid-phase endocytosis of the drug[2]. CA-074 inhibits cathepsin B with a Ki of 2 to 5 nM, whereas the initial Kis for cathepsin H and L are about 40-200 μM. CA-074 exhibits 10000-30000 times greater inhibitory effects on purified rat cathepsin B than on cathepsin H and L[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 134448-10-5
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Appearance Solid
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Molecular Weight 383.44
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Formula C18H29N3O6
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Color White to yellow
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SMILES
O=C(N1[C@@H](CCC1)C(O)=O)[C@@]([C@@H](C)CC)([H])NC([C@@H]2[C@@H](C(NCCC)=O)O2)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (30)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]2025 Dec 15;10(1):406. PMID: 41392286 -
Cell
Molecular characterization of Ebola virus glycoprotein V75A substitution in the 2018-2020 epidemic. [Abstract]2026 Feb 5;189(3):818-831.e19. PMID: 41576953 -
Nat Mater
2023 Nov;22(11):1421-1429. PMID: 37667071 -
Nat Commun
Characterization of spike glycoprotein of SARS-CoV-2 on virus entry and its immune cross-reactivity with SARS-CoV. [Abstract]2020 Mar 27;11(1):1620. PMID: 32221306 -
Autophagy
ESCRT III-mediated lysosomal repair improve renal tubular cell injury in cisplatin-induced AKI. [Abstract]2025 Mar 28. PMID: 40152606
CA-074 purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Mar 28. [Abstract]
CA074 (100 μM, 3 h) during the 24-hour cisplatin (5 μM) treatment decreased the protein expression of CTSB, BCL2, BAX, and cleaved CASP3 induced by cisplatin in BUMPT cells.
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Adv Sci (Weinh)
CCDC41 Drives Oocyte Meiotic Progression by Promoting Rab11a/Rab7-Positive Vesicle Fusion with Target Membranes. [Abstract]2025 Dec 2:e04665. PMID: 41331237
CA-074 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Dec 2:e04665. [Abstract]
CA-074 (1 μM, 6 h) rescued CCDC41 knockdown-induced abnormal spindles. The relative fluorescence intensity of MAD1/CREST was measured in Ctrl MO (n = 315), Ccdc41 MO (n = 272), and Ccdc41 MO + CA-074 oocytes (n = 299).
CA-074 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Dec 2:e04665. [Abstract]
CA-074 (1 μM, 4 h) rescued the decrease in the ratio of MAD1 to CREST induced by CCDC41 knockdown oocytes.
CA-074 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Dec 2:e04665. [Abstract]
CA-074 (1 μM, 4 h) reversed the CCDC41 knockdown-induced decrease in Cyclin B1 protein and increase in CDC20 protein.
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Adv Sci (Weinh)
2025 Aug 7:e09208. PMID: 40776529
CA-074 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Aug 7:e09208. [Abstract]
CA-074 (20 μM, 6 or 48 h) in combination with ipLNP displayed cytotoxicity in CT26 cells.
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Biomaterials
Uncloaking cell-impermeant gold nanorods via tumor microenvironmental cathepsin B facilitates cancer cell penetration and potent radiosensitization. [Abstract]2022 Dec:291:121887. PMID: 36368139 -
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Neoplasia
AXL Mediates Esophageal Adenocarcinoma Cell Invasion through Regulation of Extracellular Acidification and Lysosome Trafficking. [Abstract]2018 Oct;20(10):1008-1022. PMID: 30189359 -
Emerg Microbes Infect
Porcine deltacoronavirus resists antibody neutralization through cell-to-cell transmission. [Abstract]2023 Dec;12(1):2207688. PMID: 37125733 -
Mol Cell Proteomics
Unveiling The Peptidase Network Orchestrating Hemoglobin Catabolism in Rhodnius prolixus. [Abstract]2024 Jun;23(6):100775. PMID: 38663568 -
J Enzyme Inhib Med Chem
In-cell bioluminescence resonance energy transfer (BRET)-based assay uncovers ceritinib and CA-074 as SARS-CoV-2 papain-like protease inhibitors. [Abstract]2024 Dec;39(1):2387417. PMID: 39163165 -
PLoS Pathog
The HN protein of Newcastle disease virus induces cell apoptosis through the induction of lysosomal membrane permeabilization. [Abstract]2024 Feb 14;20(2):e1011981. PMID: 38354122 -
Int J Mol Sci
2022 Jul 7;23(14):7544. PMID: 35886900 -
Int Immunopharmacol
Genome-wide screen based on 2DG activated NLRP3 inflammasome reveals the priming signal of TLR2/4 to IKKβ but not IKKα. [Abstract]2024 Dec 9:145:113781. PMID: 39657538 -
Sci Rep
Hepatitis C virus NS3/4A inhibitors and other drug-like compounds as covalent binders of SARS-CoV-2 main protease. [Abstract]2022 Jul 16;12(1):12197. PMID: 35842458 -
Environ Toxicol
Dichloroacetate attenuates the stemness of colorectal cancer cells via trigerring ferroptosis through sequestering iron in lysosomes. [Abstract]2021 Apr;36(4):520-529. PMID: 33166055 -
Environ Toxicol
Itraconazole attenuates the stemness of nasopharyngeal carcinoma cells via triggering ferroptosis. [Abstract]2021 Feb;36(2):257-266. PMID: 32951314 -
Xenobiotica
A comparison of the activity, lysosomal stability, and efficacy of legumain-cleavable and cathepsin cleavable ADC linkers. [Abstract]2024 May 13:1-13. PMID: 38738708 -
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Solvent & Solubility
DMSO : 100 mg/mL (260.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.42 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.42 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Rats: Compound CA-074 or CA-030 or E-64 is injected intraperitoneally as a solution in saline containing DMSO. A dose of 8 mg/100 g body weight is injected. The rats are killed by a blow to the head 6 h after the injection, and their liver is perfused with saline, removed, weighed and chilled on ice. Samples of 4 g of liver are minced and homogenized. The homogenate is centrifuged at 800 xg for 15 min and the supernatant is centrifuged at 12000 xg for 30 min. The precipitate is suspended in 2 mL of 0.05 M acetate buffer, pH 5,0, and freeze-thawed for measurements of cathepsin B, H and L activities[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Towatari T, et al. Novel epoxysuccinyl peptides. A selective inhibitor of cathepsin B, in vivo. FEBS Lett. 1991 Mar 25;280(2):311-5. [Content Brief]
[2]. Montaser M, et al. CA-074, but not its methyl ester CA-074Me, is a selective inhibitor of cathepsin B within living cells. Biol Chem. 2002 Jul-Aug;383(7-8):1305-8. [Content Brief]
[3]. Yamashima T, et al. Inhibition of ischaemic hippocampal neuronal death in primates with cathepsin B inhibitor CA-074: a novel strategy for neuroprotection based on 'calpain-cathepsin hypothesis'. Eur J Neurosci. 1998 May;10(5):1723-33. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6080 mL | 13.0398 mL | 26.0797 mL | 65.1992 mL |
| 5 mM | 0.5216 mL | 2.6080 mL | 5.2159 mL | 13.0398 mL | |
| 10 mM | 0.2608 mL | 1.3040 mL | 2.6080 mL | 6.5199 mL | |
| 15 mM | 0.1739 mL | 0.8693 mL | 1.7386 mL | 4.3466 mL | |
| 20 mM | 0.1304 mL | 0.6520 mL | 1.3040 mL | 3.2600 mL | |
| 25 mM | 0.1043 mL | 0.5216 mL | 1.0432 mL | 2.6080 mL | |
| 30 mM | 0.0869 mL | 0.4347 mL | 0.8693 mL | 2.1733 mL | |
| 40 mM | 0.0652 mL | 0.3260 mL | 0.6520 mL | 1.6300 mL | |
| 50 mM | 0.0522 mL | 0.2608 mL | 0.5216 mL | 1.3040 mL | |
| 60 mM | 0.0435 mL | 0.2173 mL | 0.4347 mL | 1.0867 mL | |
| 80 mM | 0.0326 mL | 0.1630 mL | 0.3260 mL | 0.8150 mL | |
| 100 mM | 0.0261 mL | 0.1304 mL | 0.2608 mL | 0.6520 mL |
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