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Submit ReviewE 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.
分子量 | 357.41 |
公式 | C15H27N5O5 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 66701-25-5 |
PubChem ID | 123985 |
InChI Key | LTLYEAJONXGNFG-DCAQKATOSA-N |
Smiles | O=[C@@](N[C@H]([C@](NCCCCNC(N)=N)=O)CC(C)C)[C@@H]1[C@@H](C(O)=O)O1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 7.15 | 20 |
以下数据基于产品分子量 357.41。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.2 mM | 13.99 mL | 69.95 mL | 139.9 mL |
1 mM | 2.8 mL | 13.99 mL | 27.98 mL |
2 mM | 1.4 mL | 6.99 mL | 13.99 mL |
10 mM | 0.28 mL | 1.4 mL | 2.8 mL |
参考文献是支持产品生物活性的出版物。
Susa et al (2004) Human primary osteoclasts: in vitro generation and applications as pharmacological and clinical assay. J.Transl.Med. 2 6 PMID: 15025786
Bitu et al (2013) Cathepsin K is present in invasive oral tongue squamous cell carcinoma in vivo and in vitro. PLoS ONE 8 e70925 PMID: 23951042
Wadhawan et al (2014) Inhibition of cathepsin B by E-64 induces oxidative stress and apoptosis in filarial parasite. PLoS ONE 9 e93161 PMID: 24667798
Zhao et al (2010) Cytosolic FoxO1 is essential for the induction of autophagy and tumour suppressor activity. Nat.Cell.Biol. 12 665 PMID: 20543840
If you know of a relevant reference for E 64, please let us know.
关键词: E 64, E 64 supplier, E64, potent, irreversible, natural, cysteine, protease, inhibitors, inhibits, cathepsin, K, L, S, B, H, calpain, papain, Cathepsin, Calpains, Calcium-Sensitive, Proteases, 5208, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 E 64 的部分引用包括:
Lee et al (2015) Tricyclic Antidepressants amitript. and desipr. Induced Neurotoxicity Associated with Parkinson's Disease. PLoS One 38 734 PMID: 26242194
Min et al (2021) A recombinant bovine adenoviral mucosal vaccine expressing mycobacterial antigen-85B generates robust protection against tuberculosis in mice. Cell Rep Med 2 100372 PMID: 34467249
Xianglan et al (2019) 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. J Allergy Clin Immunol 144 426-441.e3 PMID: 30872118
Bénédicte et al (2023) Microglial P2X4 receptors promote ApoE degradation and contribute to memory deficits in Alzheimer's disease. Cell Mol Life Sci 80 138 PMID: 37145189
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I used the E64 in ARPE19 cells after sodium iodate administration with a fluorescent cathepsin sensor (magic red). I used E64 at 10uM and it reduced the signal of magic red vs DMSO 0.01% control