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Balicatib is a potent and selective inhibitor of cathepsin K; 10-100-fold more potent in cell-based enzyme occupancy assays than against cathepsin B, L, and S. Balicatib is the most advanced of them passed Phase II clinical trials in 2005.
| Cell Experiment | |
|---|---|
| Cell lines | Hep G2 and SMMC-7721 cells |
| Preparation method | Cell viability assay. The 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyltetrazolium bromide (MTT) assay was used to measure drug sensitivity. Briefly, Hep G2 and SMMC-7721 cells were seeded into 96-well plates (Corning, USA) at a density of 5 × 103 cells per well, incubated overnight, and then treated with various concentrations (0, 10, 20, 40, and 80 μmol/L) of baicalin for 24, 48, and 72 h. Thereafter, 20 μl of MTT solution (5 mg/mL; Sigma-Aldrich, St. Louis, MO, USA) was added to each well, and the plates were incubated at 37°C for 4 h. The formed formazan crystals were dissolved in 100 μl of DMSO after removal of the supernatant. The optical density (OD) was recorded at 490 nm using a microplate reader (Bio-Tek, Winooski, VT, USA). The percentage of cell viability was calculated as: (OD of baicalin-treated group/OD of control group) × 100%. |
| Concentrations | 0, 10, 20, 40, and 80 μmol/L |
| Incubation time | 24, 48 and 72 h |
| Animal Experiment | |
|---|---|
| Animal models | Six-week old athymic nude mice bearing Hep G2 cells xenograft model |
| Formulation | 10% DMSO and 90% propylene glycol |
| Dosages | 50 mg/kg and 100 mg/kg daily for 3 weeks |
| Administration | i.p. |
| Molecular Weight | 411.54 |
| Formula | C23H33N5O2 |
| CAS Number | 354813-19-7 |
| Solubility (25°C) | DMSO 10 mM |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Cathepsin Products |
|---|
| CAA-0225
CAA-0225 is a tissue protease L inhibitor that inhibits rat liver tissue protease L with a IC50 value of 1.9 nM. |
| Z-Gly-Pro-Arg-AMC hydrochloride
Z-Gly-Pro-Arg-AMC hydrochloride a fluorescent trypsin and cathepsin K substrate. |
| N-CBZ-Phe-Arg-AMC
N-CBZ-Phe-Arg-AMC (Z-FR-AMC) is a cathepsin substrate used in assessment activity of lysosomal cathepsin enzymes. |
| Ac-Glu-Asp(EDANS)-Lys-Pro-Ile-Leu-Phe-Phe-Arg-Leu-Gly-Lys(DABCYL)-Glu-NH2
Ac-Glu-Asp(EDANS)-Lys-Pro-Ile-Leu-Phe-Phe-Arg-Leu-Gly-Lys(DABCYL)-Glu-NH2 is a cathepsin D substrate, that can be used for cathepsin D FRET assay. |
| (S, S)-Z-FA-FMK
(S,S)-Z-FA-FMK is a cell-permeable, irreversible cathepsin B inhibitor. |
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