Home Tools

CA-074 methyl ester

Catalog No. T3420 CAS 147859-80-1

Synonyms: Cathepsin B Inhibitor IV, CA-074Me

CA-074 methyl ester (Cathepsin B Inhibitor IV) is a specific inhibitor of Cathepsin B with neuroprotective, anti-cancer, and anti-inflammatory effects.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

CA-074 methyl ester, CAS 147859-80-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 54.00
2 mg	In stock	$ 72.00
5 mg	In stock	$ 117.00
10 mg	In stock	$ 198.00
25 mg	In stock	$ 397.00
50 mg	In stock	$ 589.00
100 mg	In stock	$ 843.00
1 mL * 10 mM (in DMSO)	In stock	$ 97.00

Bulk Inquiry

Select Batch

Purity: 99.58%

Purity: 99.49%

Purity: 97.26%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	CA-074 methyl ester (Cathepsin B Inhibitor IV) is a specific inhibitor of Cathepsin B with neuroprotective, anti-cancer, and anti-inflammatory effects.
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].
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].
Kinase Assay	After seven days of cell culture and osteoclast generation, the media is removed and washed three times with PBS. BMMs are fixed with a fixing solution supplied by the manufacturer. The cells are incubated at 37°C with a solution containing deionized water, Fast Garnet GBC, Napthol phosphate, Acetate, and Tartrate for 1 h. The staining solution is removed, washed with PBS (3×), and air-dried. TRAP positive cells with three or more nuclei across whole culture area are counted as multinucleated osteoclasts using light microscopy.
Cell Research	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.(Only for Reference)

Synonyms	Cathepsin B Inhibitor IV, CA-074Me
Molecular Weight	397.47
Formula	C19H31N3O6
CAS No.	147859-80-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 73 mg/mL (183.6 mM)

H2O: 72 mg/mL (181.1 mM)

Ethanol: 73 mg/mL (183.6 mM)

References and Literature

1. Dietmar Steverding, et al. The Open Enzyme Inhibition Journal. 2011, 4:11-16. 2. Jane DT, et al. Biochem Cell Biol. 2002, 80(4):457-65.

Citations

1. Wang Y, Chen Y Y, Gao G B, et al.Polyphyllin D “Punctures” Hypertrophic Lysosomes to Reverse Drug Resistance of Hepatocellular Carcinoma by Targeting Acid Sphingomyelinase.Molecular Therapy.2023

Related compound libraries

This product is contained In the following compound libraries：

Highly Selective Inhibitor Library Anti-Neurodegenerative Disease Compound Library Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Compound Library Preclinical Compound Library Anti-Alzheimer's Disease Compound Library Covalent Inhibitor Library Immunology/Inflammation Compound Library Anti-Aging Compound Library

Related Products

Related compounds with same targets

MIV-247 Petesicatib L-006235 VBY-825 Papain Leupeptin Hemisulfate SID 26681509 Aloxistatin

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

CA-074 methyl ester 147859-80-1 Proteases/Proteasome Cysteine Protease CA074 methyl ester Inhibitor Cathepsin Cathepsin B Inhibitor IV inhibit CA 074 methyl ester CA-074Me inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.