CA-074 ME Struktur

CA-074 ME

Bezeichnung:CA-074 ME

CAS-Nr147859-80-1

Englisch Name:CA-074 ME

CBNumberCB3152175

SummenformelC19H31N3O6

Molgewicht397.47

MOL-Datei147859-80-1.mol

CA-074 ME physikalisch-chemischer Eigenschaften

Schmelzpunkt	153-155°C
Siedepunkt	666.3±55.0 °C(Predicted)
Dichte	1.212±0.06 g/cm3(Predicted)
storage temp.	-20°C
Löslichkeit	Soluble in DMSO
pka	13.38±0.40(Predicted)
Aggregatzustand	Solid
Farbe	White to Off-White
InChIKey	XGWSRLSPWIEMLQ-YTFOTSKYSA-N

Sicherheit

WGK Germany

Gefahreninformationscode (GHS)

CA-074 ME Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
CA-074 methyl ester is a cell-permeable cathepsin B inhibitor.
Verwenden
CA-074 methyl ester has been used as cathepsin B inhibitor in cardiomyocytes, HeLa cells and human pancreatic cancer PANC-1 cells.
Biologische Aktivität
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
Einzelnachweise
[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 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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