H 1152 dihydrochloride
Rho-kinase (ROCK) inhibitor that displays high selectivity over other protein kinases (IC50 values are 0.012, 0.180, 0.360, 0.745, 3.03, 5.68 and 28.3 μM for ROCKII, CAMKII, PKG, Aurora A, PKA, PKC and MLCK respectively). Inhibits sulprostone-induced contractions in guinea pig aorta (IC50 = 190 nM) and displays proerectile effects in rats.
Glycyl Derivative also available.
|Storage||Desiccate at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 392.34. 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.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.55 mL||12.74 mL||25.49 mL|
|5 mM||0.51 mL||2.55 mL||5.1 mL|
|10 mM||0.25 mL||1.27 mL||2.55 mL|
|50 mM||0.05 mL||0.25 mL||0.51 mL|
References are publications that support the products' biological activity.
Shum et al (2003) Involvement of Rho-kinase in contraction of guinea-pig aorta induced by prostanoid EP3 receptor agonist. Br.J.Pharmacol. 139 1449 PMID: 12922932
Teixeira et al (2005) Proerectile effects of the rho-kinase inhibitor (S)-(+)-2-methyl-1-[(4-methyl-5-isoquinolinyl)sulfonyl]homopiperazine (H-1152) in the rat penis. J.Pharmacol.Exp.Ther. 315 155 PMID: 15976017
Tamura et al (2005) Development of specific Rho-kinase inhibitors and their clinical application. Biochim.Biophys.Acta 1754 245 PMID: 16213195
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Keywords: H 1152 dihydrochloride, supplier, Selective, Rho-kinase, ROCK, inhibitors, inhibits, Rho-Kinase, Rho-Associated, Coiled-Coil, Kinases, p160ROCK, ROK, H1152, dihydrochloride, Rho-kinases, Rho-kinases, Tocris Bioscience
4 Citations for H 1152 dihydrochloride
Citations are publications that use Tocris products. Selected citations for H 1152 dihydrochloride include:
Augspach et al (2013) Activation of RhoA,B,C by Yersinia Cytotoxic Necrotizing Factor (CNFy) induces apoptosis in LNCaP prostate cancer cells. Toxins (Basel) 5 2241 PMID: 24284827
Sero et al (2015) Cell shape and the microenvironment regulate nuclear translocation of NF-κB in breast epithelial and tumor cells. Mol Syst Biol 11 790 PMID: 25735303
Gilsbach et al (2012) Roco kinase structures give insights into the mechanism of Parkinson disease-related leucine-rich-repeat kinase 2 mutations. Proc Natl Acad Sci U S A 109 10322 PMID: 22689969
Kramár et al (2009) Cytoskeletal changes underlie estrogen's acute effects on synaptic transmission and plasticity. J Clin Pharmacol 29 12982 PMID: 19828812
Do you know of a great paper that uses H 1152 dihydrochloride from Tocris? If so please let us know.
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