E-64 #90267
Product Information
Product Usage Information
E-64 is supplied as a lyophilized powder. For a 15 mM stock, reconstitute 5 mg of powder in 0.93 mL of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.
Storage
Store lyophilized at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.
Product Description
Molecular Weight | 357.4 g/mol |
Purity | >99% |
Molecular Formula | C15H27N5O5 |
CAS | 66701-25-5 |
Solubility | Soluble in 1:1 mixture of water or ethanol at 20 mg/mL. |
Background
The small-molecule E-64 is an anti-parasitic and anti-malarial agent that acts as an irreversible, non-selective inhibitor of cysteine proteases. E-64 binds and inhibits the cysteine proteases cathepsin K (IC50 = 1.4 nM), cathepsin S (IC50 = 4.1 nM), and cathepsin L (IC50 = 2.5 nM) in human osteoclast assays. E-64 also inhibits other proteases, including cathepsin B, cathepsin H, papain, and calpain (1,2). Exposure of filarial parasites to E-64 inhibited cathepsin B and resulted in decreased parasite motility and viability (3). E-64 effectively inhibited a SUMO-1-like cysteine protease from the African swine fever virus, resulting in impaired viral replication and a possible treatment for a viral disease that typically causes high mortality in domestic pigs (4). Inhibition of cathepsin B by E-64 in tumor cell lines reduced the invasive properties of the cells by 75% (5). E-64 treatment of ischemia-reperfusion rat kidneys blocked calpain activity and reduced several markers of renal dysfunction (6).
- Barrett, A.J. et al. (1982) Biochem J 201, 189-98.
- Susa, M. et al. (2004) J Transl Med 2, 6.
- Wadhawan, M. et al. (2014) PLoS One 9, e93161.
- Liu, B. et al. (2021) Bioorg Med Chem 35, 116055.
- Szpaderska, A.M. and Frankfater, A. (2001) Cancer Res 61, 3493-500.
- Chatterjee, P.K. et al. (2005) Biochem Pharmacol 69, 1121-31.
限制使用
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For Research Use Only. Not For Use In Diagnostic Procedures.
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