GSK 269962
Chemical Name: N-[3-[[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-1H-imidazo[4,5-c]pyridin-6-yl]oxy]phenyl]-4-[2-(4-morpholinyl)ethoxy]benzamide
Purity: ≥99%
Biological Activity
GSK 269962 is a potent Rho kinase (ROCK) inhibitor (IC50 values are 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively). Displays greater than 30-fold selectivity for ROCK against a panel of serine/threonine kinases. Induces vasorelaxation in preconstricted rat aorta (IC50 = 35 nM); lowers blood pressure in a rat model of hypertension.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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Lipopolysaccharide promotes contraction of uterine myocytes via activation of Rho/ROCK signaling pathways.
Hutchinson J, Rajagopal S, Yuan M, Norman J
FASEB J, 2014;28(1):94-105. -
Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities.
Doe et al.
J.Pharmacol.Exp.Ther., 2007;320:89 -
Discovery of aminofurazan-azabenzimidazoles as inhibitors of Rho-kinase with high kinase selectivity and antihypertensive activity.
Stavenger et al.
J.Med.Chem., 2007;50:2
Product Datasheets
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Citations for GSK 269962
The citations listed below are publications that use Tocris products. Selected citations for GSK 269962 include:
12 Citations: Showing 1 - 10
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Microglia-containing cerebral organoids derived from induced pluripotent stem cells for the study of neurological diseases.
Authors: Yiling Et al.
iScience 2023;26:106267
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Oncogenic Signaling Alters Cell Shape and Mechanics to Facilitate Cell Division under Confinement.
Authors: Buzz Et al.
Dev Cell 2020;52:563-573.e3
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A Whole Genome-Wide Arrayed CRISPR Screen in Primary Organ Fibroblasts to Identify Regulators of Kidney Fibrosis.
Authors: Hauke Et al.
SLAS Discov 2020;25:591-604
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Extracellular matrix anisotropy is determined by TFAP2C-dependent regulation of cell collisions.
Authors: Stefan Et al.
Nat Mater 2020;19:227-238
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Chemically induced neurite-like outgrowth reveals a multicellular network function in patient-derived glioblastoma cells.
Authors: Simon J Et al.
J Cell Sci 2019;132
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Methods for High-throughput Drug Combination Screening and Synergy Scoring.
Authors: Jing Et al.
Methods Mol Biol 2018;1711:351-398
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Determining the contents and cell origins of apoptotic bodies by flow cytometry.
Authors: Jiang Et al.
Sci Rep 2017;7:14444
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A high-content EMT screen identifies multiple receptor tyrosine kinase inhibitors with activity on TGFβ receptor.
Authors: Lotz-Jenne Et al.
Oncotarget 2016;7:25983
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Macrophages redirect phagocytosis by non-professional phagocytes and influence inflammation
Authors: Han Et al.
Nature 2016;539:570
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Planar cell polarity aligns osteoblast division in response to substrate strain.
Authors: Galea Et al.
Stem Cell Res Ther 2015;30:423
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Lipopolysaccharide promotes contraction of uterine myocytes via activation of Rho/ROCK signaling pathways.
Authors: Hutchinson Et al.
FASEB J 2014;28:94
-
G Protein and β-arrestin signaling bias at the ghrelin receptor.
Authors: Evron Et al.
J Biol Chem 2014;289:33442
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