Chemical Name: (2S,3S)-3-[[[(1S)-1-[[[4-(Aminoiminomethyl)amino]butyl]amino]carbonyl]-3-methylbutyl]amino]carbonyl]-2-oxiranecarboxylic acid
Biological ActivityE 64 is a potent and irreversible cysteine protease inhibitor (IC50 values are 1.4, 2.5 and 4.1 nM for cathepsin K, L and S respectively. Also inhibits papain, calpain, cathepsin B and cathepsin H. Has no effect on serine proteases. Reduces HSC-3 tongue cancer cell invasion and induces oxidative stress and apoptosis in filarial parasites. Also inhibits autophagy-associated lysosomal degradation in vitro.
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For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Human primary osteoclasts: in vitro generation and applications as pharmacological and clinical assay.
Susa et al.
Cathepsin K is present in invasive oral tongue squamous cell carcinoma in vivo and in vitro.
Bitu et al.
PLoS ONE, 2013;8:e70925
Inhibition of cathepsin B by E-64 induces oxidative stress and apoptosis in filarial parasite.
Wadhawan et al.
PLoS ONE, 2014;9:e93161
Cytosolic FoxO1 is essential for the induction of autophagy and tumour suppressor activity.
Zhao et al.
Citations for E 64
The citations listed below are publications that use Tocris products. Selected citations for E 64 include:
4 Citations: Showing 1 - 4
Microglial P2X4 receptors promote ApoE degradation and contribute to memory deficits in Alzheimer's disease.
Authors: Bénédicte Et al.
Cell Mol Life Sci 2023;80:138
A recombinant bovine adenoviral mucosal vaccine expressing mycobacterial antigen-85B generates robust protection against tuberculosis in mice.
Authors: Min Et al.
Cell Rep Med 2021;2:100372
Apolipoprotein E is a concentration-dependent pulmonary danger signal that activates the NLRP3 inflammasome and IL-1β secretion by bronchoalveolar fluid macrophages from asthmatic subjects.
Authors: Xianglan Et al.
J Allergy Clin Immunol 2019;144:426-441.e3
Tricyclic Antidepressants amitript. and desipr. Induced Neurotoxicity Associated with Parkinson's Disease.
Authors: Lee Et al.
PLoS One 2015;38:734
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