| Identification | Back Directory | [Name]
3-(4-Pyridyl)indole | [CAS]
7272-84-6 | [Synonyms]
3-(4-Pyridinyl)-
3-(4-Pyridyl)indole
3-(4-Pyridinyl)-1H-indole
1H-Indole, 3-(4-pyridinyl)-
Rho Kinase Inhibitor III, Rockout | [Molecular Formula]
C13H10N2 | [MOL File]
7272-84-6.mol | [Molecular Weight]
194.23 |
| Hazard Information | Back Directory | [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] | [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 (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. | [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 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. | [Biochem/physiol Actions]
Cell permeable: yes | [storage]
Store at -20°C | [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. |
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