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Merck

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

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A propos de cet article

Formule empirique (notation de Hill) :
C13H10N2
Numéro CAS:
Poids moléculaire :
194.23
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.54
Assay:
≥98% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
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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

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

Quality Level

storage temp.

2-8°C

Catégories apparentées

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)

Classe de stockage

11 - Combustible Solids

wgk

WGK 1


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