Quality Segment
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
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
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)
存储类别
11 - Combustible Solids
wgk
WGK 1