RKI 1447 dihydrochloride

Product Description

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.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.50 mL	12.52 mL	25.04 mL
5 mM	0.50 mL	2.50 mL	5.01 mL
10 mM	0.25 mL	1.25 mL	2.50 mL
50 mM	0.05 mL	0.25 mL	0.50 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Pireddu Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2) Med.Chem.Comm. 2013 PMID: 23275831
• Pepich 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. 2024 PMID: 39307412
• Patel RKI-1447 is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer. Cancer Res. 2012 PMID: 22846914