CA-074 ME
Synonym(s):(L-3-trans-(Propylcarbamyl)oxirane-2-carbonyl)-L -isoleucyl-L -proline methyl ester
- CAS NO.:147859-80-1
- Empirical Formula: C19H31N3O6
- Molecular Weight: 397.47
- MDL number: MFCD00797532
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-09-04 15:50:00
What is CA-074 ME?
The Uses of CA-074 ME
CA-074 methyl ester is a cell-permeable cathepsin B inhibitor.
The Uses of CA-074 ME
CA-074 methyl ester has been used as cathepsin B inhibitor in cardiomyocytes, HeLa cells and human pancreatic cancer PANC-1 cells.
What are the applications of Application
CA-074 methyl ester is a cell-permeable cathepsin B inhibitor
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.
Properties of CA-074 ME
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 |
form | Solid |
pka | 13.38±0.40(Predicted) |
color | White to Off-White |
Safety information for CA-074 ME
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for CA-074 ME
InChIKey | XGWSRLSPWIEMLQ-YTFOTSKYSA-N |
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