Catalog Number: 2414
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 also available.

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.
Additional Information
Other Product-Specific Information:
Background References
  1. Involvement of Rho-kinase in contraction of guinea-pig aorta induced by prostanoid EP3 receptor agonist.
    Shum et al.
    Br.J.Pharmacol., 2003;139:1449
  2. Proerectile effects of the rho-kinase inhibitor (S)-(+)-2-methyl-1-[(4-methyl-5-isoquinolinyl)sulfonyl]homopiperazine (H-1152) in the rat penis.
    Teixeira et al.
    J.Pharmacol.Exp.Ther., 2005;315:155
  3. Development of specific Rho-kinase inhibitors and their clinical application.
    Tamura et al.
    Biochim.Biophys.Acta, 2005;1754:245
Citations:

The citations listed below are publications that use Tocris products. Selected citations for H 1152 dihydrochloride include:

4 Citations: Showing 1 - 4
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  1. Cell shape and the microenvironment regulate nuclear translocation of NF-κB in breast epithelial and tumor cells.
    Authors: Sero Et al.
    Mol Syst Biol 2015;11:790
  2. Activation of RhoA,B,C by Yersinia Cytotoxic Necrotizing Factor (CNFy) induces apoptosis in LNCaP prostate cancer cells.
    Authors: Augspach Et al.
    Toxins (Basel) 2013;5:2241
  3. Roco kinase structures give insights into the mechanism of Parkinson disease-related leucine-rich-repeat kinase 2 mutations.
    Authors: Gilsbach Et al.
    Proc Natl Acad Sci U S A 2012;109:10322
  4. Cytoskeletal changes underlie estrogen's acute effects on synaptic transmission and plasticity.
    Authors: Kramár Et al.
    J Clin Pharmacol 2009;29:12982

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