GSK 269962
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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 57.06 | 100 | |
| ethanol | 5.71 | 10mM 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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Product Datasheets
References
References are publications that support the products' biological activity.
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, supplier, glaxosmithkline, rock, rho, kinases, rock1, rock2, potent, selective, inhibitors, inhibits, antihypertensive, hypotensive, GSK269962, Rho-kinases, Rho-kinases, Tocris Bioscience
2 Citations for GSK 269962
Citations are publications that use Tocris products. Selected citations for GSK 269962 include:
Han et al (2016) Macrophages redirect phagocytosis by non-professional phagocytes and influence inflammation Nature 539 570 PMID: 27820945
Galea et al (2015) Planar cell polarity aligns osteoblast division in response to substrate strain. Stem Cell Res Ther 30 423 PMID: 25264362
Do you know of a great paper that uses GSK 269962 from Tocris? If so please let us know.
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