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 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 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|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
Baicalin induces apoptosis in hepatic cancer cells in vitro and suppresses tumor growth in vivo.
Yu Y, et al. Int J Clin Exp Med. 2015 Jun 15;8(6):8958-67. PMID: 26309548.
Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.
Falgueyret JP,et al. J Med Chem. 2005 Dec 1;48(24):7535-43. PMID: 16302795.
|Related Cathepsin Products|
UK-371804 is a potent and selective urokinase-type plasmogen activator (uPA) inhibitor with excellent enzyme potency (Ki=10 nM) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin).
Odanacatib (MK-0822) is an inhibitor of cathepsin K, an enzyme involved in bone resorption.
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