product name E-64
Description: E-64, isolated from cultures of Aspergillus, is an irreversible and selective cysteine protease inhibitor with IC50 of 9 nM for papain. E-64 was shown to inhibit papain, ficin and the fruit and stem bromelains, with disappearance of the thiol group of papain. E-64 has been reported to inhibit two other mammalian cysteine proteinases: cathepsin L and a proteinase from human breast-tumour tissue and the calcium-dependent proteinase, calpain, from chicken muscle. All of these characteristics suggested that E-64 might be a valuable inhibitor for the study of cysteine proteinases.
References: Biopolymers. 1999;51(1):99-107; J Egypt Soc Parasitol. 2009 Apr;39(1):111-9.
357.41
Formula
C15H27N5O5
CAS No.
66701-25-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 71 mg/mL (198.7 mM)
Water: <1 mg/mL
Ethanol: 11 mg/mL (30.8 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19409606
| In Vitro |
In vitro activity: E-64 rapidly inhibits the activities of the cysteine proteinases cathepsins B, H and L and papain, while has no effect on the serine proteinases or the metalloproteinases. E-64, as a specific inhibitor os cysteine proteases, effectively blocks in vitro ovarian cancer cell invasion. In addition, E-64 also shows antiparasitic activity against Giardia lamblia excystation in vitro. E-64 improves the preimplantation development of bovine somatic cell nuclear transfer embryos, which indicates another important implication of E-64. Kinase Assay: Cell Assay: E-64 inhibited H-59 invasion in a dose-dependent manner with a maximal inhibition of 97% at a concentration of 10 μg/ml which was non-toxic. Cell migration as measured with filters coated with 7.5 μg/filter type IV collagen was reduced by only 25% suggesting that the cysteine proteinases played a more minor role in cell migration in the absence of a basement membrane barrier. On the other hand M-27 invasion was not significantly affected by treatment with E-64 even at concentrations as high as 100 μg/ml. |
|---|---|
| In Vivo | E-64 induces a marked decrease in the number of spontaneous metastasis in M5076 tumor bearing mice, while has no effect on the formation of experimental metastasis. E-64 also shows antiparasitic activity against Giardia lamblia excystation in infected mice. |
| Animal model | Wistar strain rats |
| Formulation & Dosage | 1 mg/100 g body weight; i.p. injection |
| References | Biopolymers. 1999;51(1):99-107; J Egypt Soc Parasitol. 2009 Apr;39(1):111-9; J Biochem. 1982 Apr;91(4):1373-80. |
