Synonyms: compound 2b [PMID: 8765519] | E-64d | E64d | EP453 | loxistatin
Compound class:
Synthetic organic
Comment: Aloxistatin (EP-453) is an irreversible inhibitor of the cysteine protease cathepsin B and calpains 1 and 2 [2]. It acts by alkylating the catalytic cysteine thiol [1]. In cellular assays it inhibits autophagy and lysosomal function.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
|
References |
1. Barrett AJ, Kembhavi AA, Brown MA, Kirschke H, Knight CG, Tamai M, Hanada K. (1982)
L-trans-Epoxysuccinyl-leucylamido(4-guanidino)butane (E-64) and its analogues as inhibitors of cysteine proteinases including cathepsins B, H and L. Biochem J, 201 (1): 189-98. [PMID:7044372] |
2. Meara JP, Rich DH. (1996)
Mechanistic studies on the inactivation of papain by epoxysuccinyl inhibitors. J Med Chem, 39 (17): 3357-66. [PMID:8765519] |
3. Méthot N, Rubin J, Guay D, Beaulieu C, Ethier D, Reddy TJ, Riendeau D, Percival MD. (2007)
Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing. J Biol Chem, 282 (29): 20836-46. [PMID:17535802] |