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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.
Sold for research purposes under agreement from GlaxoSmithKline.
Compound Libraries for GSK 269962
Technical Data for GSK 269962
|Storage||Store at +4°C|
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|
|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|
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
6 Citations for GSK 269962
Citations are publications that use Tocris products. Selected citations for GSK 269962 include:
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
Galea et al (2015) Planar cell polarity aligns osteoblast division in response to substrate strain. Stem Cell Res Ther 30 423 PMID: 25264362
Jiang et al (2017) Determining the contents and cell origins of apoptotic bodies by flow cytometry. Sci Rep 7 14444 PMID: 29089562
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
Do you know of a great paper that uses GSK 269962 from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Stem Cells Scientific Review
Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.
Stem Cell Workflow Poster
Stem cells have potential as a source of cells and tissues for research and treatment of disease. This poster summarizes some key protocols demonstrating the use of small molecules across the stem cell workflow, from reprogramming, through self-renewal, storage and differentiation to verification. Advantages of using small molecules are also highlighted.