GSK 269962

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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)
Datasheet
Citations (12)
Reviews
Literature (3)

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.

Select a batch to recalculate based on the batch molecular weight:
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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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.

View Related Products by Product Action

View all Rho-Kinase Inhibitors

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

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

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


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Reviews for GSK 269962

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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

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 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.

Stem Cells Poster

Stem Cells Poster

Written by Rebecca Quelch and Stefan Przyborski from Durham University (UK), this poster describes the isolation of pluripotent stem cells, their maintenance in culture, differentiation, and the generation and potential uses of organoids.