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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 76739-51-0
- 分子式: C14H25N3O5
- 分子量:315.37
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
Cathepsin アイソフォーム固有の製品をすべて表示
More
生物活性
製品説明
IC50 & Target
[1]|
papain 0.4 μg/mL (IC50) |
体外実験
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:ICR mice (male, seven-week-old)[1]
-
Dosage:500 μg
-
Administration:i.p.; daily; 8 consecutive days
-
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.
化学情報
-
CAS 番号 76739-51-0
-
分子量 315.37
-
分子式 C14H25N3O5
-
SMILES
C(N[C@H](C(NCCCCN)=O)CC(C)C)(=O)[C@@H]1[C@@H](C(O)=O)O1
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)