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3-(4-Pyridyl)indole (Synonyms: Rho Kinase Inhibitor III,ROCK Inhibitor III,Rockout)

Katalog-Nr.GC12314

3-(4-Pyridyl)indol (Rockout) ist ein Rho-Kinase (ROCK)-Hemmer mit einem IC50 von 25 μM.

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3-(4-Pyridyl)indole Chemische Struktur

Cas No.: 7272-84-6

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

3-(4-pyridyl)indole (Rockout) is a Rho-kinase inhibitor [1].

Rho-associated protein kinase (ROCK) belongs to a family of serine-threonine kinases mainly involved in regulating the shape and movement of cells by acting on the cytoskeleton [2].

Rockout caused decreased migration and aberrant morphology. Rockout showed no effect on phagocytosis, listeria motility or actin polymerization in permeabilized yeast. In a human melanoma cell line M2 cells that blebs constitutively in a manner that is sensitive to actin cytoskeletal perturbation, Rockout (50 μM) stopped the cell blebbing within 2 min and with washout blebbing returned to normal levels within 3 min. The IC50 of Rockout was 12 μM and it inhibited blebbing in nearly all cells at 50 μM. In B3T3 cells, treatment with 50 μM Rockout resulted in significant morphological change within 10 min [1]. At an ATP concentration of 100 μM, Rockout inhibited ROCK activity with an approximate IC50 of 25 μM. Rockout (25 μM) inhibited ROCK-II and PRK to a similar degree, and MSK-1 and PKA to a lesser extent. Rockout showed no inhibitory effect on PKCα or SAPK2a [1].

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.

Chemical Properties

Cas No. 7272-84-6 SDF
Überlieferungen Rho Kinase Inhibitor III,ROCK Inhibitor III,Rockout
Chemical Name 3-(4-pyridinyl)-1H-indole
Canonical SMILES C12=CC=CC=C1NC=C2C3=CC=NC=C3
Formula C13H10N2 M.Wt 194.2
Löslichkeit ≤30mg/ml in ethanol;20mg/ml in DMSO;30mg/ml in dimethyl formamide Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 5.1493 mL 25.7467 mL 51.4933 mL
5 mM 1.0299 mL 5.1493 mL 10.2987 mL
10 mM 0.5149 mL 2.5747 mL 5.1493 mL
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