Submit a Review & Earn an Amazon Gift Card
You can now submit reviews for your favorite Tocris products. Your review will help other researchers decide on the best products for their research. Why not submit a review today?!
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 |
Molarity Calculator
Molarity Calculator
Calculate the mass, volume, or concentration required for a solution.
Reconstitution Calculator
Reconstitution Calculator
Dilution Calculator
Dilution Calculator
Calculate the dilution required to prepare a stock solution.
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
If you know of a relevant reference for RKI 1447 dihydrochloride, please let us know.
View Related Products by Target
View Related Products by Product Action
Keywords: RKI 1447 dihydrochloride, RKI 1447 dihydrochloride supplier, RKI1447, dihydrochloride, Potent, and, selective, ROCK, inhibitors, inhibits, anti-invasive, antitumor, breast, cancer, ROCK1, ROCK2, MLC-2, MYPT-1, in, vivo, Rho-kinases, 5061, Tocris Bioscience
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
Do you know of a great paper that uses RKI 1447 dihydrochloride from Tocris? Please let us know.
Reviews for RKI 1447 dihydrochloride
There are currently no reviews for this product. Be the first to review RKI 1447 dihydrochloride and earn rewards!
Have you used RKI 1447 dihydrochloride?
Submit a review and receive an Amazon gift card.
$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image
$25/€18/£15/$25CAN/¥75 Yuan/¥2500 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image
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!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Stem Cells Scientific Review
Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.
Stem Cell Workflow Poster
Stem cells have potential as a source of cells and tissues for research and treatment of disease. This poster summarizes some key protocols demonstrating the use of small molecules across the stem cell workflow, from reprogramming, through self-renewal, storage and differentiation to verification. Advantages of using small molecules are also highlighted.
Stem Cells Poster
Written by Rebecca Quelch and Stefan Przyborski from Durham University (UK), this poster describes the isolation of pluripotent stem cells, their maintenance in culture, differentiation, and the generation and potential uses of organoids.