Product nameE-64, cysteine protease inhibitor
DescriptionIrreversible, selective, potent cysteine protease inhibitor
- N-(trans-Epoxysuccinyl)-L-leucine 4-guanidinobutylamide
Irreversible, potent, and selective cysteine protease inhibitor (IC50 values for cathepsins K, S, and L, in vitro, are 1.4, 4.1, and 2.5 nM, respectively). Does not inhibit serine proteases (except trypsin).
Chemical name(2R,3R)-3-[[(2S)-1-[4-(Diaminomethylideneamino)butylamino]-4-methyl-1-oxopentan-2-yl]carbamoyl]oxirane-2-carboxylic acid
Storage instructionsStore at -20°C. Store under desiccating conditions. The product can be stored for up to 12 months.
Solubility overviewSoluble in water to 50 mM and in DMSO to 50 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
This product has been referenced in:
- Susa M et al. Human primary osteoclasts: in vitro generation and applications as pharmacological and clinical assay. J Transl Med 2:6 (2004). Read more (PubMed: 15025786) »
- Navab R et al. Inhibition of carcinoma cell invasion and liver metastases formation by the cysteine proteinase inhibitor E-64. Clin Exp Metastasis 15:121-9 (1997). Read more (PubMed: 9062388) »
- Sreedharan SK et al. Demonstration that 1-trans-epoxysuccinyl-L-leucylamido-(4-guanidino) butane (E-64) is one of the most effective low Mr inhibitors of trypsin-catalysed hydrolysis. Characterization by kinetic analysis and by energy minimization and molecular dynamics simulation of the E-64-beta-trypsin complex. Biochem J 316 ( Pt 3):777-86 (1996). Read more (PubMed: 8670152) »
- Lampi KJ et al. Comparison of cell-permeable calpain inhibitors and E64 in reduction of cataract in cultured rat lenses. Toxicol Appl Pharmacol 117:53-7 (1992). Read more (PubMed: 1440613) »
- Barrett AJ et al. 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 201:189-98 (1982). Read more (PubMed: 7044372) »
- Hashida S et al. Inhibitions by E-64 derivatives of rat liver cathepsin B and cathepsin L in vitro and in vivo. J Biochem 88:1805-11 (1980). Read more (PubMed: 7462205) »