CA 074 (Synonyms: CA-074,CA074) |
Katalog-Nr.GC16317
One-Click Copy Product Info
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CA 074 is a selective inhibitor of cathepsin B with a Ki value of 2-5 nM. CA 074 is 10000-30000 times more potent against purified rat cathepsin B than against cathepsin H and L.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 134448-10-5
Sample solution is provided at 25 µL, 10mM.
CA 074 is a selective inhibitor of cathepsin B with a Ki value of 2-5 nM. CA 074 is 10000-30000 times more potent against purified rat cathepsin B than against cathepsin H and L[1]. CA 074 is a synthetic analog of E-64, a natural peptidyl epoxide that irreversibly inhibits most lysosomal cysteineproteases[2]. CA 074 cannot cross cell membranes, but its methyl ester form, CA-074 Me (GC15917), can cross cell membranes[3].
In vitro, CA 074 (10 μM) treatment of HT29, DLD1, and SW480 cells for 2-3 weeks significantly inhibited cell invasion through Matrigel by approximately 45-60% [4].
In vivo, CA 074 (10 mg/kg) treated intravenously in mice inoculated with human melanoma cells significantly inhibited tumor growth and the number of lung metastases [5]. CA 074 (50 mg/kg) was injected intraperitoneally into 4T1.2 tumor-bearing mice, which significantly inhibited tumor growth, reduced tumor cathepsin B activity, and inhibited lung and bone metastasis[6]. CA 074 (4 mg/kg) was injected intravenously into rats with focal cerebral ischemia, which significantly reduced the levels of cathepsin B and L and increased the number of eosinophilic (necrotic) and apoptotic neurons in brain tissue[7].
References:
[1] Towatari T, Nikawa T, Murata M, et al. Novel epoxysuccinyl peptides A selective inhibitor of cathepsin B, in vivo[J]. FEBS letters, 1991, 280(2): 311-315.
[2] Matsumoto K, Mizoue K, Kitamura K, et al. Structural basis of inhibition of cysteine proteases by E‐64 and its derivatives[J]. Peptide Science, 1999, 51(1): 99-107.
[3] Patel N, Nizami S, Song L, et al. CA‐074Me compound inhibits osteoclastogenesis via suppression of the NFATc1 and c‐FOS signaling pathways[J]. Journal of Orthopaedic Research, 2015, 33(10): 1474-1486.
[4] Bian B, Mongrain S, Cagnol S, et al. Cathepsin B promotes colorectal tumorigenesis, cell invasion, and metastasis[J]. Molecular carcinogenesis, 2016, 55(5): 671-687.
[5] Matarrese P, Ascione B, Ciarlo L, et al. Cathepsin B inhibition interferes with metastatic potential of human melanoma: an in vitro and in vivo study[J]. Molecular cancer, 2010, 9: 1-14.
[6] Withana N P, Blum G, Sameni M, et al. Cathepsin B inhibition limits bone metastasis in breast cancer[J]. Cancer research, 2012, 72(5): 1199-1209.
[7] Özkara E, Durmaz R, Özbek Z, et al. The Effect of Ca-074 (Cathepsın B Inhibitor) on Necrotic and Apoptotic Neuronal Cell Death in Model of Cerebral Ischemia[J]. Osmangazi Tıp Dergisi, 2023, 45(5): 781-790.
| Cell experiment [1]: | |
Cell lines | HT29, DLD1, SW480 cells |
Preparation Method | HT29, DLD1, and SW480 cells were cultured in soft agarose in the presence or absence of 10 μM CA 074 for 2–3 week. |
Reaction Conditions | 10μM; 2–3 week |
Applications | CA 074 significantly inhibited cell invasion through Matrigel by approximately 45–60%. |
| Animal experiment [2]: | |
Animal models | CD-1 male nude (nu/nu) mice |
Preparation Method | MM4 cells were injected into the hind leg muscle of mice. Beginning on day 6 after tumor implantation (tumor mass approximately 250mg), mice were treated with CA 074 at 10 mg/kg intravenously for eight consecutive days. |
Dosage form | 10mg/kg; i.v. |
Applications | CA 074 significantly inhibited tumor growth and suppressed the number of metastases in artificial lungs. |
References: | |
| Cas No. | 134448-10-5 | SDF | |
| Überlieferungen | CA-074,CA074 | ||
| Chemical Name | (2S)-1-[(2S,3S)-3-methyl-2-[[(3S)-3-(propylcarbamoyl)oxirane-2-carbonyl]amino]pentanoyl]pyrrolidine-2-carboxylic acid | ||
| Canonical SMILES | CCCNC(=O)C1C(O1)C(=O)NC(C(C)CC)C(=O)N2CCCC2C(=O)O | ||
| Formula | C18H29N3O6 | M.Wt | 383.44 |
| Löslichkeit | ≥ 19.17mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.608 mL | 13.0398 mL | 26.0797 mL |
| 5 mM | 521.6 μL | 2.608 mL | 5.2159 mL |
| 10 mM | 260.8 μL | 1.304 mL | 2.608 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)