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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 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) 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. 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 |
|---|
| N-Ethylmaleimide
N-Ethylmaleimide (NEM) is a cysteine protease inhibitor. |
| Odanacatib
Odanacatib (MK-0822) is a potent and reversible covalent inhibitor of CathepsinK (CatK) with an IC50 of 0.2 nM/1 nM for human/rabbit cathepsin B, L, and S and is highly selective. |
| Aloxistatin
Aloxistatin (E64d) is an irreversible and membrane-permeable cysteine protease inhibitor. |
| Cathepsin Inhibitor 1
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. |
| Loxistatin Acid
Loxistatin Acid (E-64C), a derivative of E-64, is an irreversible and membrane-permeant cysteine protease inhibitor. |
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