RKI 1447 dihydrochloride

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Cat.No. 5061 - RKI 1447 dihydrochloride | C16H14N4O2S.2HCl
Description: Potent and selective ROCK inhibitor; antitumor
Chemical Name: N-[(3-Hydroxyphenyl)methyl]-N'-[4-(4-pyridinyl)-2-thiazolyl]urea dihydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations
Literature

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.

Select a batch to recalculate based on the batch molecular weight:
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

Safety Datasheet

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


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Citations for RKI 1447 dihydrochloride

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Cardiovascular

Cardiovascular Research Product Guide

A collection of over 250 products for cardiovascular research, the guide includes research tools for the study of:

  • Hypertension
  • Thrombosis and Hemostasis
  • Atherosclerosis
  • Myocardial Infarction
  • Ischemia/Reperfusion Injury
  • Arrhythmias
  • Heart Failure
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases

Pathways for RKI 1447 dihydrochloride

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