CA-074 ME Property

Melting point:

153-155°C

Boiling point:

666.3±55.0 °C(Predicted)

Density 

1.212±0.06 g/cm3(Predicted)

storage temp. 

-20°C

solubility 

Soluble in DMSO

pka

13.38±0.40(Predicted)

form 

Solid

color 

White to Off-White

InChIKey

XGWSRLSPWIEMLQ-YTFOTSKYSA-N

Safety

WGK Germany 

3

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

CA-074 ME Chemical Properties,Usage,Production

Uses

CA-074 methyl ester is a cell-permeable cathepsin B inhibitor.

Uses

CA-074 methyl ester has been used as cathepsin B inhibitor in cardiomyocytes, HeLa cells and human pancreatic cancer PANC-1 cells.

Biological Activity

ca-074 me is a membrane-permeable and selective inhibitor of cathepsin b with ic50 value of 36.3 nm [1, 2].ca-074 me is a methyl ester derivative of ca-074. in cultured human gingival fibroblasts, ca-074 me exerted a 95% inhibition of cathepsin b and partial inhibition (54%) of the combined activities of cathepsins b and l. ca-074 me was also found to inhibit cathespin l under reducing conditions. it inhibited the activity of purified human cathepsin l by more than 90% when the enzyme had been pre-incubated with 1.4 mm dtt or 4.2 mm gsh for 2 hours. besides that, ca-074 me completely inhibited cathepsin b in the presence of 1.4 mm dtt [2, 3].

Biochem/physiol Actions

CA-074 methyl ester is a cell-permeable analog of CA-074. It is an inhibitor of cathepsin B especially the intracellular type. and undergoes intracellular transition into active CA-074 by the action of esterases. CA-074 methyl ester also inhibits cathepsin L.

target

cathepsin B

References

[1] wu x, zhang l, gurley e, et al. prevention of free fatty acid–induced hepatic lipotoxicity by 18β-glycyrrhetinic acid through lysosomal and mitochondrial pathways. hepatology, 2008, 47(6): 1905-1915.
[2] steverding d. the cathepsin b-selective inhibitors ca-074 and ca-074me inactivate cathepsin l under reducing conditions. open enzyme inhibition journal, 2011, 4: 11-16.
[3] buttle d j, murata m, knight c g, et al. ca074 methyl ester: a proinhibitor for intracellular cathepsin b. archives of biochemistry and biophysics, 1992, 299(2): 377-380.