CA-074 methyl ester (CA-074 Me)

Catalog No.S7420 Synonyms: Cathepsin B Inhibitor IV

For research use only.

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

CAS No. 147859-80-1

Selleck's CA-074 methyl ester (CA-074 Me) has been cited by 19 publications

Purity & Quality Control

Choose Selective Cathepsin B Inhibitors

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

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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF-10A neoT NYXaV4pYTnWwY4Tpc44h[XO|YYm= NH\QNXYzKGi{cx?= NV3Td5puUW6qaXLpeIlwdiCxZjDjZZRp\XC|aX6gRkBqdiCqdX3hckBOS0ZvMUDBJI5md1RiY3XscJMh[XO|ZYPz[YQh[XNicILveIVwdHm|aYOgc4Yh\Xi2cnHj[YxtfWyjcjDt[Y1jemGwZTDifUBu\WG|dYLpcoch\GWlcnXhd4UhcW5iaX70doFk\WyudXzhdkBl\We{YXTheIlwdiCxZjDEVU1kd2yuYXflckA1KGG2IEWwJJVOKGmwY4XiZZRm\CCob4KgNkBpenNiZn;scI94\WRiYomgSHEu[2:ubHHn[Y4h[WSmaYTpc44hdWWjc4Xy[YQh\m:{IEKgbJJ{Ng>? MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTVyM{CyOEc,Ojl3MEOwNlQ9N2F-
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].

Protocol (from reference)

Cell Research:[1]
  • 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.
Animal Research:[3]
  • 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).

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 397.47
Formula

C19H31N3O6

CAS No. 147859-80-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCCNC(=O)C1C(O1)C(=O)NC(C(C)CC)C(=O)N2CCCC2C(=O)OC

In vivo Formulation Calculator (Clear solution)

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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 ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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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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