147859-80-1 Usage
Description
CA-074 ME, also known as CA-074 methyl ester, is a cell-permeable cathepsin B inhibitor derived from natural sources. It possesses the ability to inhibit the activity of cathepsin B, a lysosomal protease enzyme, which plays a crucial role in various biological processes.
Uses
Used in Pharmaceutical Applications:
CA-074 ME is used as a cathepsin B inhibitor for its potential therapeutic applications in various diseases. By inhibiting cathepsin B, it can help modulate cellular processes and pathways, making it a promising candidate for drug development.
Used in Research Applications:
CA-074 ME is used as a cathepsin B inhibitor in various cell types, including cardiomyocytes, HeLa cells, and human pancreatic cancer PANC-1 cells. It serves as a valuable tool for researchers to study the role of cathepsin B in cellular processes and its potential involvement in disease progression.
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.
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.
Check Digit Verification of cas no
The CAS Registry Mumber 147859-80-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,4,7,8,5 and 9 respectively; the second part has 2 digits, 8 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 147859-80:
(8*1)+(7*4)+(6*7)+(5*8)+(4*5)+(3*9)+(2*8)+(1*0)=181
181 % 10 = 1
So 147859-80-1 is a valid CAS Registry Number.
