H 1152 dihydrochloride

Cat. No. 2414

H 1152 dihydrochloride C16H21N3O2S.2HCl [871543-07-6]

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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. Glycyl derivative available (Cat. No. 2485).

Technical Data

M.Wt:
392.34
Formula:
C16H21N3O2S.2HCl
Solubility:
Soluble to 100 mM in water and to 50 mM in DMSO
Purity:
>98 %
Storage:
Desiccate at +4°C
CAS No:
871543-07-6

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

Certificate of Analysis / Product Datasheet
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References are publications that support the products' biological activity.

Tamura et al (2005) Development of specific Rho-kinase inhibitors and their clinical application. Biochim.Biophys.Acta 1754 245. PMID: 16213195.

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.

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.

If you know of a relevant reference for H 1152 dihydrochloride please let us know.

Citations are publications that use Tocris products. Selected citations for H 1152 dihydrochloride include:

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.

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.

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.show all ▼show less ▲

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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, Tocris Bioscience, Rho-Kinases Inhibitor products

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