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Submit ReviewGSK 269962
Description: Potent and selective ROCK inhibitor
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% (HPLC)
Biological Activity for GSK 269962
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.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline.
Compound Libraries for GSK 269962
GSK 269962 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
Technical Data for GSK 269962
| M. Wt | 570.6 |
| Formula | C29H30N8O5 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 850664-21-0 |
| PubChem ID | 16095342 |
| InChI Key | YOVNFNXUCOWYSG-UHFFFAOYSA-N |
| Smiles | CCN(C(C4=NON=C4N)=N3)C1=C3C=NC(OC2=CC(NC(C5=CC=C(OCCN6CCOCC6)C=C5)=O)=CC=C2)=C1 |
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.
Solubility Data for GSK 269962
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 57.06 | 100 | |
| ethanol | 5.71 | 10 with gentle warming |
Preparing Stock Solutions for GSK 269962
The following data is based on the product molecular weight 570.6. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.75 mL | 8.76 mL | 17.53 mL |
| 5 mM | 0.35 mL | 1.75 mL | 3.51 mL |
| 10 mM | 0.18 mL | 0.88 mL | 1.75 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.35 mL |
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Product Datasheets for GSK 269962
References for GSK 269962
References are publications that support the biological activity of the product.
Doe et al (2007) Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. J.Pharmacol.Exp.Ther. 320 89 PMID: 17018693
Stavenger et al (2007) Discovery of aminofurazan-azabenzimidazoles as inhibitors of Rho-kinase with high kinase selectivity and antihypertensive activity. J.Med.Chem. 50 2 PMID: 17201404
If you know of a relevant reference for GSK 269962, please let us know.
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Keywords: GSK 269962, GSK 269962 supplier, glaxosmithkline, rock, rho, kinases, rock1, rock2, potent, selective, inhibitors, inhibits, antihypertensive, hypotensive, GSK269962, Rho-kinases, 4009, Tocris Bioscience
12 Citations for GSK 269962
Citations are publications that use Tocris products. Selected citations for GSK 269962 include:
Jiang et al (2017) Determining the contents and cell origins of apoptotic bodies by flow cytometry. Sci Rep 7 14444 PMID: 29089562
Galea et al (2015) Planar cell polarity aligns osteoblast division in response to substrate strain. Stem Cell Res Ther 30 423 PMID: 25264362
Simon J et al (2019) Chemically induced neurite-like outgrowth reveals a multicellular network function in patient-derived glioblastoma cells. J Cell Sci 132 PMID: 31515278
Jing et al (2018) Methods for High-throughput Drug Combination Screening and Synergy Scoring. Methods Mol Biol 1711 351-398 PMID: 29344898
Lotz-Jenne et al (2016) A high-content EMT screen identifies multiple receptor tyrosine kinase inhibitors with activity on TGFβ receptor. Oncotarget 7 25983 PMID: 27036020
Han et al (2016) Macrophages redirect phagocytosis by non-professional phagocytes and influence inflammation Nature 539 570 PMID: 27820945
Evron et al (2014) G Protein and β-arrestin signaling bias at the ghrelin receptor. J Biol Chem 289 33442 PMID: 25261469
Hutchinson et al (2014) Lipopolysaccharide promotes contraction of uterine myocytes via activation of Rho/ROCK signaling pathways. FASEB J 28 94 PMID: 24076962
Yiling et al (2023) Microglia-containing cerebral organoids derived from induced pluripotent stem cells for the study of neurological diseases. iScience 26 106267 PMID: 36936782
Buzz et al (2020) Oncogenic Signaling Alters Cell Shape and Mechanics to Facilitate Cell Division under Confinement. Dev Cell 52 563-573.e3 PMID: 32032547
Stefan et al (2020) Extracellular matrix anisotropy is determined by TFAP2C-dependent regulation of cell collisions. Nat Mater 19 227-238 PMID: 31659294
Hauke et al (2020) A Whole Genome-Wide Arrayed CRISPR Screen in Primary Organ Fibroblasts to Identify Regulators of Kidney Fibrosis. SLAS Discov 25 591-604 PMID: 32425084
Do you know of a great paper that uses GSK 269962 from Tocris? Please let us know.
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