GSK 269962

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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 (6)
Reviews
Literature (6)

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. 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

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


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Literature in this Area

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