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GSK 269962

Cat. No. 4009 5 Citations Submit a Review Datasheet / COA / SDS
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Cat.No. 4009 - GSK 269962 | C29H30N8O5 | CAS No. 850664-21-0
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 (5)
Reviews
Literature
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

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

GSK 269962 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 57.06 100
ethanol 5.71 10 with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 570.6. Batch specific molecular weights may vary from batch to batch due to solvent 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

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

5 Citations for GSK 269962

Citations are publications that use Tocris products. Selected citations for GSK 269962 include:

Galea et al (2015) Planar cell polarity aligns osteoblast division in response to substrate strain. Stem Cell Res Ther 30 423 PMID: 25264362

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

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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