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A cell-permeable indolopyridine compound that acts as a selective, ATP-competitive inhibitor of Rho kinase (ROCK) activity

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]

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 (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 ROCK2 and PRK2, another Rho-dependent kinase, with similar potency, while inhibiting MSK-1 and PKA with relatively weaker potency.

ChEBI:3-pyridin-4-yl-1H-indole is a member of indoles.

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.

Cell permeable: yes

Store at -20°C

[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.