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CA-074 Me

selective and cell-permeable cathepsin B inhibitor

CA-074 Me

Catalog No. A8239
Size Price Stock Qty
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.

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Chemical structure

CA-074 Me

Related Biological Data

CA-074 Me

Related Biological Data

CA-074 Me

Biological Activity

Description CA-074 Me is a selective and cell-permeable inhibitor of cathepsin B.
Targets cathepsin B          
IC50 2.2 nM          

Protocol

Cell experiment: [1]

Cell lines

McNtcp.24 cells

Preparation method

This product is soluble in DMSO. Stock solution can be stored at -80 °C less than 6 months.

Reacting condition

0.1 µM, 2 hours

Applications

Cells were incubated in medium alone or with 50 µM GCDC in the absence or presence of 0.1 µM CA-074 Me. Apoptosis was quantitated after 2 h of incubation. The cathepsin B inhibitor CA-074 Me reduced the GCDC-mediated increase in cathepsin B activity and apoptosis in McNtcp.24 cells. The result confirms that cathepsin B activity increases and contributes to bile salt–mediated apoptosis in primary rat hepatocytes.

Animal experiment: [2]

Animal models

CatB+/+ mice

Dosage form

Intraperitoneal injection, 4 mg/100g

Application

Serum ALT levels after TNF-α-treatment were significantly reduced in catB+/+ mice pretreated with CA-074 Me compared to saline-injected controls. In contrast, liver architecture was preserved and only moderate damage was observed in catB+/+ mice pretreated with CA-074 Me. These results suggest that pharmacological inhibition of cat B may partially attenuate TNF-α-induced liver damage.

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] Faubion W A, Guicciardi M E, Miyoshi H, et al. Toxic bile salts induce rodent hepatocyte apoptosis via direct activation of Fas. The Journal of clinical investigation, 1999, 103(1): 137-145.

[2] Guicciardi M E, Miyoshi H, Bronk S F, et al. Cathepsin B knockout mice are resistant to tumor necrosis factor-α-mediated hepatocyte apoptosis and liver injury: implications for therapeutic applications. The American journal of pathology, 2001, 159(6): 2045-2054.

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Chemical Properties

Cas No. 147859-80-1 SDF Download SDF
Chemical Name methyl (2S)-1-[(2S)-3-methyl-2-[[(2S,3S)-3-(propylcarbamoyl)oxirane-2-carbonyl]amino]pentanoyl]pyrrolidine-2-carboxylate
Canonical SMILES CCCNC(=O)C1C(O1)C(=O)NC(C(C)CC)C(=O)N2CCCC2C(=O)OC
Formula C19H31N3O6 M.Wt 397.5
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

Background

A cell-permeable analog of CA-074 that acts as an irreversible inhibitor of intracellular cathepsin B. Reported to inhibit bone resorption in rodent models and shown to inhibit B16 melanoma cell invasion in vitro.