555553

Rho Kinase Inhibitor III, Rockout

The Rho Kinase Inhibitor III, Rockout, also referenced under CAS 7272-84-6, controls the biological activity of Rho Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonyme(s) : Rho Kinase Inhibitor III, Rockout, 3-(4-Pyridyl)-1H-indole
• Formule empirique (notation de Hill) : C₁₃H₁₀N₂
• Numéro CAS: 7272-84-6
• Poids moléculaire : 194.23
• MDL number: MFCD01035958
• UNSPSC Code: 12352200
• NACRES: NA.54
• Assay: ≥98% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Propriétés

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: yellow
• solubility: DMSO: 25 mg/mL, methanol: soluble
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: [nH]1c2c(c(c1)c3ccncc3)cccc2
• InChI: 1S/C13H10N2/c1-2-4-13-11(3-1)12(9-15-13)10-5-7-14-8-6-10/h1-9,15H
• InChI key: LLJRXVHJOJRCSM-UHFFFAOYSA-N

Description

General description

A cell-permeable indolopyridine compound that acts as a selective, reversible, and ATP-competitive inhibitor of Rho kinase activity with an IC₅₀ of 25 µM. Does not inhibit the activation of Rho kinase nor does it affect the in vitro activities of MLCK, PKCα, and SAPK2a/p38α. Shown to be 5-fold less potent than Y-27632 (Cat. No. 688000; IC₅₀ = ~5 µM), and display a similar specificity profile as H-89 (Cat. No. 371963). Affects cell migration, inhibits blebbing (IC₅₀ = ~ 12 µM in M2 cells), and decreases stress fibers in Bulb 3T3 cells at 50 µM.

A cell-permeable, selective, reversible, and ATP-competitive inhibitor of Rho kinase activity (IC₅₀ = 25 µM). Does not inhibit the activation of Rho kinase nor does it affect the in vitro activities of MLCK, PKCα, and SAPK2a/p38α. Shown to be 5-fold less potent than Y-27632 (Cat. No. 688000; IC₅₀ ~5 µM), and display a similar specificity profile as H-89 (Cat. No. 371963). Affects cell migration, inhibits blebbing (IC₅₀ ~12 µM in M2 cells), and decreases stress fibers in Bulb 3T3 cells at 50 µM.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
ROCK

Product competes with ATP.

Reversible: yes

Target IC₅₀: 25 µM against ROCK

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Yarrow, J.C., et al. 2005. Chem. Biol.12, 385.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Informations sur la sécurité

• Classe de stockage: 11 - Combustible Solids
• Que se passe-t-il ?: WGK 1