Home Proteases Cathepsin B inhibitor - Cysteine Protease inhibitor CA-074 methyl ester (CA-074 Me) For research use only.

CA-074 methyl ester (CA-074 Me)

Synonyms: Cathepsin B Inhibitor IV

CA-074 methyl ester (CA-074 Me, Cathepsin B Inhibitor IV) is a membrane-permeable derivative of CA-074 and acts as an irreversible cathepsin B inhibitor.

CA-074 methyl ester (CA-074 Me) Chemical Structure

CA-074 methyl ester (CA-074 Me) Chemical Structure

CAS No. 147859-80-1

Purity & Quality Control

Batch: S742001 DMSO]79 mg/mL]false]Ethanol]79 mg/mL]false]Water]2.5 mg/mL]false Purity: 99.55%
99.55

CA-074 methyl ester (CA-074 Me) Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF-10A neoT Function assay 2 hrs Inhibition of cathepsin B in human MCF-10A neoT cells assessed as proteolysis of extracellular membrane by measuring decrease in intracellular degradation of DQ-collagen 4 at 50 uM incubated for 2 hrs followed by DQ-collagen addition measured for 2 hrs. 29503024
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Biological Activity

Description CA-074 methyl ester (CA-074 Me, Cathepsin B Inhibitor IV) is a membrane-permeable derivative of CA-074 and acts as an irreversible cathepsin B inhibitor.
Targets
Cathepsin B [1]
In vitro
In vitro CA-074Me is able to inhibit cathepsin L within living HL-60 cells and bloodstream forms of Trypanosoma brucei brucei, but does not inhibit cathepsin L in the absence of thiols. CA-074Me is converted into CA-074 by intracellular esterasesand is, therefore, able to inhibit cathepsin B in GSH-depleted HL-60 cell. It is suggested that CA-074 rather than CA-074Me should be used to selectively inhibit cathespsin B within living cells[1]. Myotube size and number and induced levels of fusion-related creatine phosphokinase activity and myosin heavy-chain protein are reduced from 30 to 50% in CA074Me-treated myoblasts. These reductions are also dose related. Micromolar concentrations of CA074Me inhibit catB activity in differentiating myoblasts[2].
Cell Research Cell lines HL-60 cells
Concentrations 100 μM
Incubation Time 2 h
Method HL-60 cells are pre-treated for 24 h with 200 μM BSO followed by 60 min with 1 mM DEM. Thereafter, the cells(1×106/ml) are incubated with 100 μM CA-074 or CA-074Me, in the presence of 1% DMSO, 200 μM BSO and 1 mM DEM at 37°C. Control cultures are treated with 1% DMSO alone or with 100 μM Z-FA-DMK in the presence of 200 μM BSO and 1 mM DEM. Untreated HL-60 cells are incubated with 100 μM CA-074 or CA-074Me, in the presence of 1% DMSO at 37°C. Untreated control cultures are incubated with 1% DMSO alone or with 100 μM Z-FA-DMK. After 2 h incubation, cells are washed three times with PBS/1% glucose and lysed in 100 mM citrate, pH 5.0, 2% Chaps (106 cells/100 μl). Subsequently, the lysate is centrifuged and the clarified supernatant used to assay for proteolytic activity.
In Vivo
In vivo Administration of CA074Me to the London APP mice results in significant improvement in memory deficit, reduces amyloid plaque load in brain, reduces levels of Aβ40 and Aβ42 in brain, and reduces C-terminal β-secretase fragment (CTFβ) derived from APP by β-secretase when compared with untreated control animals. It has no effect on any of these parameters in mice expressing the Swe mutant β-secretase site of APP (in Swedish/London APP mice). In vivo icv administration of CA074Me to normal guinea pigs results in substantial reduction of brain Aβ levels and inhibits β-secretase activity[3].
Animal Research Animal Models London APP mice
Dosages 1 mg/ml
Administration An ALZET osmotic minipump was implanted subcutaneously in the midscapular area of the back of each animal. A catheter was connected to the osmotic minipump and inserted into the lateral ventricle of the brain (icv).

Chemical Information & Solubility

Molecular Weight 397.47 Formula

C19H31N3O6
CAS No. 147859-80-1 SDF Download CA-074 methyl ester (CA-074 Me) SDF
Smiles CCCNC(=O)C1C(O1)C(=O)NC(C(C)CC)C(=O)N2CCCC2C(=O)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 79 mg/mL ( (198.75 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 79 mg/mL

Water : 2.5 mg/mL


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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