Description
Two Rho-associated kinases (ROCK), ROCK1 and ROCK2, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal. 3-(4-Pyridyl)indole is a ROCK1 inhibitor (IC
50 = 25 μM) that promotes cell spreading, inhibits membrane blebbing, and induces dissolution of actin stress fibers in a wound healing assay. It also inhibits ROCK2 and PRK2, another Rho-dependent kinase, with similar potency, while inhibiting MSK-1 and PKA with relatively weaker potency.
Chemical Properties
Yellow Solid
Uses
A cell-permeable indolopyridine compound that acts as a selective, ATP-competitive inhibitor of Rho kinase (ROCK) activity.
Uses
Two Rho-associated kinases (ROCK), ROCK-I and ROCK-II, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal. 3-(4-Pyridyl)indole is a ROCK-I inhibitor (IC50 = 25 μM) that promotes cell spreading, inhibits membrane blebbing, and induces dissolution of actin stress fibers in a wound healing assay. It also inhibits ROCK-II and PRK2, another Rho-dependent kinase, with similar potency, while inhibiting MSK-1 and PKA with relatively weaker potency.[Cayman Chemical]
Definition
ChEBI: 3-pyridin-4-yl-1H-indole is a member of indoles.
General Description
A cell-permeable indolopyridine compound that acts as a selective, reversible, and ATP-competitive inhibitor of Rho kinase activity with an IC
50 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; IC
50 = ~5 μM), and display a similar specificity profile as H-89 (Cat. No. 371963). Affects cell migration, inhibits blebbing (IC
50 = ~ 12 μM in M2 cells), and decreases stress fibers in Bulb 3T3 cells at 50 μM.
Biochem/physiol Actions
Cell permeable: yes
References
[1] yarrow j c, totsukawa g, charras g t, et al. screening for cell migration inhibitors via automated microscopy reveals a rho-kinase inhibitor[j]. chemistry & biology, 2005, 12(3): 385-395.
[2] amano m, fukata y, kaibuchi k. regulation and functions of rho-associated kinase[j]. experimental cell research, 2000, 261(1): 44-51.
