GSK 269962

Name: GSK 269962
Brand: Tocris Bioscience
SKU: 4009

Tocris Bioscience a Bio-Techne Brand

Catalog # 4009

Citations (6)

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Key Product Details

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)
Molecular Weight:	570.6

View Full Technical Details for GSK 269962

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 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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References for GSK 269962

References are publications that support the biological activity of the product.

Doe Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. J.Pharmacol.Exp.Ther. 2007 PMID: 17018693
Stavenger Discovery of aminofurazan-azabenzimidazoles as inhibitors of Rho-kinase with high kinase selectivity and antihypertensive activity. J.Med.Chem. 2007 PMID: 17201404

Citations for GSK 269962 (6)

Showing 1 - 6 of 6 citations Showing All

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Citations are publications that use Bio-Techne 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
Han et al. (2016) Macrophages redirect phagocytosis by non-professional phagocytes and influence inflammation Nature. 539:570
PMID: 27820945
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
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

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