Biological Activity
Potent and selective ROCK inhibitor (IC50 values are 6.2 and 14.5 nM for ROCK2 and ROCK1 respectively); suppresses phosphorylation of ROCK substrates MLC-2 and MYPT-1 in human cancer cells, but has no effect on the phosphorylation levels of Akt, MEK, and S6 kinase. Displays anti-invasive and antitumor activities in breast cancer cells.
Compound Libraries
RKI 1447 dihydrochloride is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 399.29 |
| Formula | C16H14N4O2S.2HCl |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| PubChem ID | 90489001 |
| InChI Key | GBXLRAPHQIRDNS-UHFFFAOYSA-N |
| Smiles | O=C(NCC3=CC=CC(O)=C3)NC1=NC(C2=CC=NC=C2)=CS1.Cl.Cl |
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 | 39.93 | 100 | |
| water | 3.99 | 10mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 399.29. 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 | 2.5 mL | 12.52 mL | 25.04 mL |
| 5 mM | 0.5 mL | 2.5 mL | 5.01 mL |
| 10 mM | 0.25 mL | 1.25 mL | 2.5 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Patel et al (2012) RKI-1447 is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer. Cancer Res. 72 5025 PMID: 22846914
Pireddu et al (2013) Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2) Med.Chem.Comm. 3 699 PMID: 23275831
Keywords: RKI 1447 dihydrochloride, supplier, RKI1447, dihydrochloride, Potent, and, selective, ROCK, inhibitors, inhibits, anti-invasive, antitumor, breast, cancer, ROCK1, ROCK2, MLC-2, MYPT-1, Rho-kinases, Rho-kinases, Tocris Bioscience
