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Category: EnzymesarrowKinasesarrowRho-kinases
Cat.No. Product Name
2414

H 1152 dihydrochloride

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H 1152 2HCl
Chemical Name: (S)-(+)-2-Methyl-1-[(4-methyl-5-isoquinolinyl)sulfonyl] -hexahydro-1H-1,4-diazepine dihydrochloride

Biological Activity:

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.

Technical Data:

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M.Wt: 392.34
Formula: C16H21N3O2S.2HCl
Storage: Desiccate at +4°C
Solubility: Soluble to 100 mM in Water and to 50 mM in DMSO
Purity: >98%
CAS No: [451462-58-1]

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    References:

    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. 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. Tamura et al (2005) Development of specific Rho-kinase inhibitors and their clinical application. Biochim.Biophys.Acta 1754 245.
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    Keywords: H 1152 2HCl, Kinases, Selective Rho-kinase (ROCK) Inhibitor, H1152 2HCl, Tocris Bioscience
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