Description: Potent and irreversible cysteine protease inhibitor
Chemical Name: (2S,3S)-3-[[[(1S)-1-[[[4-(Aminoiminomethyl)amino]butyl]amino]carbonyl]-3-methylbutyl]amino]carbonyl]-2-oxiranecarboxylic acid
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
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.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
water
7.15
20
Preparing Stock Solutions
The following data is based on the product molecular weight 357.41. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
2.8 mL
13.99 mL
27.98 mL
5 mM
0.56 mL
2.8 mL
5.6 mL
10 mM
0.28 mL
1.4 mL
2.8 mL
50 mM
0.06 mL
0.28 mL
0.56 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Susaet al (2004) Human primary osteoclasts: in vitro generation and applications as pharmacological and clinical assay. J.Transl.Med. 2 6 PMID: 15025786
Bituet al (2013) Cathepsin K is present in invasive oral tongue squamous cell carcinoma in vivo and in vitro. PLoS ONE 8 e70925 PMID: 23951042
Wadhawanet al (2014) Inhibition of cathepsin B by E-64 induces oxidative stress and apoptosis in filarial parasite. PLoS ONE 9 e93161 PMID: 24667798
Zhaoet al (2010) Cytosolic FoxO1 is essential for the induction of autophagy and tumour suppressor activity. Nat.Cell.Biol. 12 665 PMID: 20543840