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| CA-074 ME Basic information |
| Product Name: | CA-074 ME | | Synonyms: | N-(L-3-TRANS-PROPYLCARBONYL-OXIRANE-2-CARBONYL)-L-ISOLEUCYL-L-PROLINE METHYL ESTER;L-trans-Epoxysuccinyl(propylamide)-Ile-P;(L-3-Trans-(propylcarbamoyl)oxirane-2-carbony;L-trans-Epoxysuccinic Ile-Pro-OMe Propylamide;L-trans-Epoxysuccinyl-isoleucyl-proline methyl ester propylamide;CA-074 methyl ester;(L-3-trans-(Propylcarbamyl)oxirane-2-carbonyl)-L-isoleucyl-L-proline methyl ester;CA-074(OME) | | CAS: | 147859-80-1 | | MF: | C19H31N3O6 | | MW: | 397.47 | | EINECS: | | Product Categories: | peptides;Pepetides | | Mol File: | 147859-80-1.mol |
| CA-074 ME Chemical Properties |
| 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 |
| CA-074 ME Usage And Synthesis |
| 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. | | 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. |
| CA-074 ME Preparation Products And Raw materials |
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