RKI 1447 dihydrochloride

Name: RKI 1447 dihydrochloride
Brand: Tocris Bioscience
SKU: 5061

Tocris Bioscience, part of Bio-Techne | Catalog # 5061

Citations (2)

COA / SDS

Potent and selective ROCK inhibitor; antitumor

Key Product Details

Description:	Potent and selective ROCK inhibitor; antitumor
Chemical Name:	N-[(3-Hydroxyphenyl)methyl]-N'-[4-(4-pyridinyl)-2-thiazolyl]urea dihydrochloride
Purity:	≥98% (HPLC)
Molecular Weight:	399.29

View Full Technical Details for RKI 1447 dihydrochloride

Technical Data
Citations

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	≥98% (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 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	2.50 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

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References for RKI 1447 dihydrochloride

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