|Cathepsin B inhibitor|
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
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|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.|
|Cas No.||134448-10-5||SDF||Download SDF|
|Chemical Name||(2S)-1-[(2S,3S)-3-methyl-2-[[(3S)-3-(propylcarbamoyl)oxirane-2-carbonyl]amino]pentanoyl]pyrrolidine-2-carboxylic acid|
|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
CA-074 is better-suited for cathepsin B specific inactivation in living cells, since it selectively inhibited cathepsin B leaving cathepsin L unaffected.
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.
CA-074 was used to inhibit cathepsin B activity in order to measure cathepsin L activity in samples.
CA-074, a specific cathepsin B inhibitor, also abolished the neurotoxic effects caused by Abeta42-activated BV2 cell . 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 . 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 . 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.  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.
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)