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Sigma-Aldrich

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.

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Synonym(s):
Rho Kinase Inhibitor III, Rockout, 3-(4-Pyridyl)-1H-indole
Empirical Formula (Hill Notation):
C13H10N2
CAS Number:
Molecular Weight:
194.23
UNSPSC Code:
12352200
NACRES:
NA.54

Quality Level

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

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

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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

WGK

WGK 1


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