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Submit ReviewRKI 1447 dihydrochloride
Description: Potent and selective ROCK inhibitor; antitumor
Chemical Name: N-[(3-Hydroxyphenyl)methyl]-N'-[4-(4-pyridinyl)-2-thiazolyl]urea dihydrochloride
Purity: ≥99% (HPLC)
Biological Activity for RKI 1447 dihydrochloride
RKI 1447 dihydrochloride is a 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. RKI 1447 dihydrochloride enhances the efficacy of BET inhibitors on the downregulation of N-Myc in vitro and in vivo.
Compound Libraries for RKI 1447 dihydrochloride
RKI 1447 dihydrochloride 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 RKI 1447 dihydrochloride
| M. Wt | 399.29 |
| Formula | C16H14N4O2S.2HCl |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 1782109-09-4 |
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for RKI 1447 dihydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 3.99 | 10 with gentle warming | |
| DMSO | 39.93 | 100 |
Preparing Stock Solutions for RKI 1447 dihydrochloride
The following data is based on the product molecular weight 399.29. 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 | 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 |
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Product Datasheets for RKI 1447 dihydrochloride
References for RKI 1447 dihydrochloride
References are publications that support the biological activity of the product.
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
Pepich et al (2024) The ROCK-1/2 inhibitor RKI-1447 blocks N-MYC, promotes cell death, and emerges as a synergistic partner for BET inhibitors in neuroblastoma. Cancer Lett. PMID: 39307412
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1 Citation for RKI 1447 dihydrochloride
Citations are publications that use Tocris products. Selected citations for RKI 1447 dihydrochloride include:
Pepich et al (2024) The ROCK-1/2 inhibitor RKI-1447 blocks N-MYC, promotes cell death, and emerges as a synergistic partner for BET inhibitors in neuroblastoma. Cancer Lett. PMID: 39307412
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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