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5.33982

Dock5 Inhibitor, C21

Name: Dock5 Inhibitor, C21
Brand: MM

别名:

Dock5 Inhibitor, C21, N-(3,5-Dichlorophenyl)benzenesulfonamide

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关于此项目

经验公式（希尔记法）:

C₁₂H₉Cl₂NO₂S

化学文摘社编号:

54129-15-6

分子量:

302.18

MDL number:

MFCD01212617

UNSPSC Code:

12352200

NACRES:

NA.77

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

Storage condition:

OK to freeze, protect from light

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属性

assay

≥98% (HPLC)

Quality Level

100

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

说明

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
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.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c