EP-459
EP-459 is a papain inhibitor (IC50=0.4 μg/mL) with no significant inhibitory activity against serine proteases such as trypsin, plasmin, thrombin, and urokinase. The effects of EP-459 are similar to those of E-64C (HY-100227), but differ from the functions of leupeptin and its analogs. EP-459 can serve as a titration reagent for mouse cathepsin L (precursor form/MEP) activity, covalently binding to the cysteine residue at its active site. EP-459 is also a Ca2+-dependent active site-directed inhibitor that can inactivate chicken gizzard smooth muscle calpain II, and can be acetylated to generate Ac-Ep-459, which after radiolabeling can be used to prepare [3H]Ac-Ep-459 for calpain active site labeling.
For research use only. We do not sell to patients.
- CAS No.: 76739-51-0
- Formula: C14H25N3O5
- Molecular Weight:315.37
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
papain 0.4 μg/mL (IC50) |
In Vitro
EP-459 inhibits purified papain with an IC50 of 0.4 μg/mL, and does not inhibit trypsin, plasmin, thrombin, or urokinase at concentrations up to 100 μg/mL[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice (male, seven-week-old)[1]
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Dosage:500 μg
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Administration:i.p.; daily; 8 consecutive days
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Result:Measured proline aminopeptidase activity at 0.85 nmol per min per mg protein, formyl methionine aminopeptidase activity at 4.21 nmol per min per mg protein, phenylalanine aminopeptidase activity at 3.86 nmol per min per mg protein, Gly-Pro-Leu-AP activity at 0.55 nmol per min per mg protein, α-D-mannosidase activity at 0.17 nmol per min per mg protein, N-Ac-β-D-glucosaminidase activity at 0.42 nmol per min per mg protein, esterase activity at 34.59 nmol per min per mg protein, AP-A activity at 0.44 nmol per min per mg protein, AP-B activity at 5.51 nmol per min per mg protein, leucine aminopeptidase activity at 3.25 nmol per min per mg protein, trypsin-like enzyme activity at 18.05 nmol per min per mg protein, chymotrypsin-like enzyme activity at 21.37 nmol per min per mg protein, elastase-like enzyme activity at 17.77 nmol per min per mg protein, cathepsin C activity at 0.42 nmol per min per mg protein, α-D-glucosidase activity at 0.51 nmol per min per mg protein, creatine kinase activity at 27.24 nmol per min per mg protein, and phosphatase activity at 1.63 nmol per min per mg protein in forelimb muscle.
Measured cathepsin C activity at 2.40 nmol per min per mg protein, N-Ac-β-D-glucosaminidase activity at 0.56 nmol per min per mg protein, elastase-like enzyme activity at 25.80 nmol per min per mg protein, AP-A activity at 4.93 nmol per min per mg protein, AP-B activity at 7.09 nmol per min per mg protein, proline aminopeptidase activity at 1.54 nmol per min per mg protein, leucine aminopeptidase activity at 7.41 nmol per min per mg protein, formyl methionine aminopeptidase activity at 10.09 nmol per min per mg protein, phenylalanine aminopeptidase activity at 7.33 nmol per min per mg protein, Gly-Pro-Leu-AP activity at 3.24 nmol per min per mg protein, trypsin-like enzyme activity at 16.35 nmol per min per mg protein, chymotrypsin-like enzyme activity at 22.68 nmol per min per mg protein, α-D-glucosidase activity at 1.74 nmol per min per mg protein, α-D-mannosidase activity at 1.45 nmol per min per mg protein, phosphatase activity at 3.29 nmol per min per mg protein, and esterase activity at 944 nmol per min per mg protein in liver.
Clustered closely with E-64C and clearly differentiated from leupeptin and its analogues in in vivo enzymatic activity changes across all six tested organs via multivariate principal component analysis.
Chemical Information
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CAS No. 76739-51-0
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Molecular Weight 315.37
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Formula C14H25N3O5
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SMILES
C(N[C@H](C(NCCCCN)=O)CC(C)C)(=O)[C@@H]1[C@@H](C(O)=O)O1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
EP-459 Related Classifications
HY-187732 Related Classifications
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