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CA 074

Cathepsin B inhibitor

CA 074

Catalog No. A1926
Size Price Stock Qty
Evaluation Sample $28.00 In stock
1mg $55.00 In stock
5mg $150.00 In stock
10mg $250.00 In stock
25mg $400.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Chemical structure

CA 074

Related Biological Data

CA 074

Related Biological Data

CA 074

Biological Activity

Inhibitor of cathepsin B (Ki = 2-5 nM). Displays selectivity over cathepsins H and L (Ki = 40-200 μM). Shown to reduce bone metastasis in a 4T1.2 breast cancer model.
Targets cathepsin B          
Ki 2-5nM          

Protocol

Cell experiment [1]:

Cell lines

Human umbilical vein endothelial cells (HUVECs)

Preparation method

This product is soluble in DMSO mostly at 20 mM. It is also soluble in ethanol with 20 mM.

Reacting condition

24 h; 10 mM

Applications

The effects on the viability of HUVECs of cathepsin B specific inhibitors 10 mM CA-074 (96.9±1.2% viability ) and its membrane-permeable analog CA-074-Me (101.7±0.4% viability) was negligible, as was that of Minocycline (102.3±2.6% ) at 10mM.

Animal experiment [2]:

Animal models

Female Balb/c mice

Dosage form

50 mg/kg; intraperitoneal injection

Application

To test the therapeutic efficacy of cysteine protease inhibitors in vivo, we treated 4T1.2 tumor –bearing mice with the selective CA-074 inhibitor. Treatment of 4T1.2 tumor–bearing mice with the inhibitor had no impact on primary tumor growth. However, analysis of metastasis revealed a significant difference between in the compounds. CA-074 treatment significantly decreased metastasis to lung (P < 0.05) and bone (P < 0.05).

Other notes

Please 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] Premzl A, Turk V, Kos J. Intracellular proteolytic activity of cathepsin B is associated with capillary‐like tube formation by endothelial cells in vitro[J]. Journal of cellular biochemistry, 2006, 97(6): 1230-1240.

[2] 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.

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Chemical Properties

Cas No. 134448-10-5 SDF Download SDF
Synonyms 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
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition: Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

View Related Products By Research Topics

Research Update

1. 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.
Abstract
CA-074 is better-suited for cathepsin B specific inactivation in living cells, since it selectively inhibited cathepsin B leaving cathepsin L unaffected.
2. 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.
Abstract
Intravenous administration of CA-074 exhibited excellent inhibition against cathepsin B and saved CA1 neurons from delayed neuronal death in monkeys undergoing a complete 20 min whole brain ischaemia.

Background

CA-074, a specific cathepsin B inhibitor, also abolished the neurotoxic effects caused by Abeta42-activated BV2 cell [1]. Co-treatment of cultures with the cathepsin B inhibitors CA-074 or Z-FA-FMK suppressed the cytostatic effects of TPA and activation of pro-uPA [2]. Administration of CA-074 suppresses the response to exogenous antigens, such as hepatitis B virus antigen, ovalbumin and Leishmania major antigen, and induces switching of the helper T cell responses from Th-2 to Th-1 of CD4+ T cell, thereby down regulating the production of IgE and IgG1 [3]. Pharmacological inhibition of cat B in catB(+/+) mice with L-3-trans-(propylcarbamoyl)oxirane-2-carbonyl-Lisoleucyl-L-proline (CA-074 Me) also reduced TNF-alpha-induced liver damage. [4] Administration of cathepsin B inhibitors, E-64, CA-074 and vitamin B6, caused the strong suppression of the Th-2 type immune responses .

 Inhibitor of cathepsin B (Ki = 2-5 nM). Displays selectivity over cathepsins H and L (Ki = 40-200 μM). Shown to reduce bone metastasis in a 4T1.2 breast cancer model.

References:
1. Identification of cathepsin B as a mediator of neuronal death induced by Abeta-activated microglial cells using a functional genomics approach. Gan, L., Ye, S., Chu, A., Anton, K., Yi, S., Vincent, V.A., von Schack, D., Chin, D., Murray, J., Lohr, S., Patthy, L., Gonzalez-Zulueta, M., Nikolich, K., Urfer, R. J. Biol. Chem. (2004)
2. Phorbol ester activation of a proteolytic cascade capable of activating latent transforming growth factor-betaL a process initiated by the exocytosis of cathepsin B. Guo, M., Mathieu, P.A., Linebaugh, B., Sloane, B.F., Reiners, J.J. J. Biol. Chem. (2002)
3. Insights into the roles of cathepsins in antigen processing and presentation revealed by specific inhibitors. Katunuma, N., Matsunaga, Y., Himeno, K., Hayashi, Y. Biol. Chem. (2003)
4. Cathepsin B knockout mice are resistant to tumor necrosis factor-alpha-mediated hepatocyte apoptosis and liver injury: implications for therapeutic applications. Guicciardi, M.E., Miyoshi, H., Bronk, S.F., Gores, G.J. Am. J. Pathol. (2001)