DOCK5 INHIBITOR C21 1PC X 50MG

General description

A cell-permeable, bioavailable, non-toxic benzenesulfonamide compound that directly blocks Dock5-mediated Rac activation (k_cat/K_M = 7.9 x 10⁴ & 9.5 x 10⁴ M^-1s^-1 for Rac1 & Rac2 by Dock5-DHR2, respectively) with selectivity over RhoA and Cdc42. At higher concentrations, affects Dock1 and Dock2 guanine nucleotide exchange factor activity. Shown to reversibly perturb podosome organization and inhibit osteoclastic bone degradation in a dose-dependent manner. Efficiently prevents both arthritis and metastasis-induced bone loss while preserving bone formation in several osteolytic disease mouse model (25 mg/kg, i.p. or i.v., 5 days a week for 4 weeks). Unlike alendronate (Cat. No. 126855), C21 does not impair bone formation.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

A cell-permeable, bioavailable, non-toxic benzenesulfonamide compound that directly blocks Dock5-mediated Rac activation (k_cat/K_M = 7.9 x 10⁴ & 9.5 x 10⁴ M^-1s^-1 for Rac1 & Rac2 by Dock5-DHR2, respectively) with selectivity over RhoA and Cdc42. At higher concentrations, affects Dock1 and Dock2 guanine nucleotide exchange factor activity. Shown to reversibly perturb podosome organization and inhibit osteoclastic bone degradation in a dose-dependent manner. Efficiently prevents both arthritis and metastasis-induced bone loss while preserving bone formation in several osteolytic disease mouse model (25 mg/kg, i.p. or i.v., 5 days a week for 4 weeks). Unlike alendronate (Cat. No. 126855), C21 does not impair bone formation.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
Dock5

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Vives, V., et al. 2015. Nat. Commun.6, 6218.
Vives, V., et al. 2011. J. Bone Miner. Res.26, 1099.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany