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Cathepsin Inhibitor 1

Cat. No. M2497
Cathepsin Inhibitor 1 Structure
Size Price Availability Quantity
5mg USD 120  USD120 In stock
10mg USD 190  USD190 In stock
25mg USD 380  USD380 In stock
50mg USD 660  USD660 In stock
100mg USD 1020  USD1020 In stock
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Quality Control & Documentation
Biological Activity

Cathepsin Inhibitor 1 is an inhibitor of Cathepsin (L, L2, S, K, B) with pIC50 of 7.9, 6.7, 6.0, 5.5 and 5.2, respectively.

Product Citations
Customer Product Validations & Biological Datas
Source Oncotarget (2017). Figure 3. Cathepsin inhibitor 1 (AbMole BioScience, Shanghai, China)
Method MTT assay
Cell Lines SGC-7901 and GES-1 cells
Concentrations 122 μM
Incubation Time 2 h
Results As shown in Figure 3E, the cathepsin inhibitor 1, an inhibitor of Cathepsin L, Cathepsin L2, Cathepsin S, Cathepsin K and Cathepsin B, could not reduce hispidin-induced cell death. This indicates that cathepsins were not the real driver of the process.
Chemical Information
Molecular Weight 401.89
Formula C20H24ClN5O2
CAS Number 225120-65-0
Form Solid
Solubility (25°C) DMSO 70 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Zahira Tber, et al. Selective inhibition of human cathepsin S by 2,4,6-trisubstituted 1,3,5-triazine analogs

[2] Steingrimur Stefansson, et al. Mutants of plasminogen activator inhibitor-1 designed to inhibit neutrophil elastase and cathepsin G are more effective in vivo than their endogenous inhibitors

[3] J Duranton, et al. DNA strongly impairs the inhibition of cathepsin G by alpha(1)-antichymotrypsin and alpha(1)-proteinase inhibitor

[4] J Duranton, et al. Kinetic mechanism of the inhibition of cathepsin G by alpha 1-antichymotrypsin and alpha 1-proteinase inhibitor

[5] P J Hogg, et al. Thrombospondin 1 is a tight-binding competitive inhibitor of neutrophil cathepsin G. Determination of the kinetic mechanism of inhibition and localization of cathepsin G binding to the thrombospondin 1 type 3 repeats

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Keywords: Cathepsin Inhibitor 1 supplier, Cathepsin, inhibitors, activators


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