5.33982
Dock5 Inhibitor, C21
Synonym(s):
Dock5 Inhibitor, C21, N-(3,5-Dichlorophenyl)benzenesulfonamide
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About This Item
Empirical Formula (Hill Notation):
C12H9Cl2NO2S
CAS Number:
Molecular Weight:
302.18
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light
assay
≥98% (HPLC)
Quality Segment
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
gray
solubility
DMSO: 50 mg/mL
storage temp.
2-8°C
SMILES string
[S](=O)(=O)(Nc2cc(cc(c2)Cl)Cl)c1ccccc1
InChI
1S/C12H9Cl2NO2S/c13-9-6-10(14)8-11(7-9)15-18(16,17)12-4-2-1-3-5-12/h1-8,15H
InChI key
HMKZVAZQKOKXRZ-UHFFFAOYSA-N
General description
A cell-permeable, bioavailable, non-toxic benzenesulfonamide compound that directly blocks Dock5-mediated Rac activation (kcat/KM = 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
Dock5
Preparation Note
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.
Vives, V., et al. 2011. J. Bone Miner. Res.26, 1099.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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