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Submit ReviewH 1152 dihydrochloride
Description: Selective Rho-kinase (ROCK) inhibitor
Chemical Name: (S)-(+)-2-Methyl-1-[(4-methyl-5-isoquinolinyl)sulfonyl]-hexahydro-1H-1,4-diazepine dihydrochloride
Purity: ≥98% (HPLC)
Biological Activity for H 1152 dihydrochloride
H 1152 dihydrochloride is a 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 for H 1152 dihydrochloride
| M. Wt | 392.34 |
| Formula | C16H21N3O2S.2HCl |
| Storage | Desiccate at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 871543-07-6 |
| PubChem ID | 11560225 |
| InChI Key | BFOPDSJOLUQULZ-GXKRWWSZSA-N |
| Smiles | CC1=CN=CC2=C1C(S(N3CCCNC[C@@H]3C)(=O)=O)=CC=C2.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 Data for H 1152 dihydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 39.23 | 100 | |
| DMSO | 19.62 | 50 |
Preparing Stock Solutions for H 1152 dihydrochloride
The following data is based on the product molecular weight 392.34. 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 | 2.55 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 |
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Product Datasheets for H 1152 dihydrochloride
References for H 1152 dihydrochloride
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for H 1152 dihydrochloride, please let us know.
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Keywords: H 1152 dihydrochloride, H 1152 dihydrochloride supplier, Selective, Rho-kinase, ROCK, inhibitors, inhibits, Rho-Kinase, Rho-Associated, Coiled-Coil, Kinases, p160ROCK, ROK, H1152, dihydrochloride, Rho-kinases, 2414, Tocris Bioscience
16 Citations for H 1152 dihydrochloride
Citations are publications that use Tocris products. Selected citations for H 1152 dihydrochloride include:
Messal et al (2019) Tissue curvature and apicobasal mechanical tension imbalance instruct cancer morphogenesis. Nature 566 126 PMID: 30700911
Sero and Bakal (2017) Multiparametric Analysis of Cell Shape Demonstrates that β-PIX Directly Couples YAP Activation to Extracellular Matrix Adhesion. Cell Syst 4 84 PMID: 28065575
Durkin et al (2017) RhoD Inhibits RhoC-ROCK-Dependent Cell Contraction via PAK6. Dev Cell 41 315 PMID: 28486133
Rath et al (2017) ROCK signaling promotes collagen remodeling to facilitate invasive pancreatic ductal adenocarcinoma tumor cell growth. EMBO Mol Med 9 198 PMID: 28031255
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
Zenker et al (2018) Expanding Actin Rings Zipper the Mouse Embryo for Blastocyst Formation. Cell 173 776 PMID: 29576449
Aoun et al (2016) Anoctamin 6 Contributes to Cl- Secretion in Accessory Cholera Enterotoxin (Ace)-stimulated Diarrhea: AN ESSENTIAL ROLE FOR PHOSPHATIDYLINOSITOL 4,5-BISPHOSPHATE (PIP2) SIGNALING IN CHOLERA. J Biol Chem 291 26816 PMID: 27799301
Rath et al (2018) Rho Kinase Inhibition by AT13148 Blocks Pancreatic Ductal Adenocarcinoma Invasion and Tumor Growth. Cancer Res 78 3321 PMID: 29669760
Pitha et al (2018) Rho-Kinase Inhibition Reduces Myofibroblast Differentiation and Proliferation of Scleral Fibroblasts Induced by Transforming Growth Factor β and Experimental Glaucoma. Transl Vis Sci Technol 7 6 PMID: 30479877
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
Berenjeno et al (2017) Oncogenic PIK3CA induces centrosome amplification and tolerance to genome doubling. Nat Commun 8 1773 PMID: 29170395
Schipper et al (2019) Rebalancing of actomyosin contractility enables mammary tumor formation upon loss of E-cadherin. Nat Commun 10 3800 PMID: 31444332
García-Morales et al (2019) Sp1-regulated expression of p11 contributes to motor neuron degeneration by membrane insertion of TASK1. Nat Commun 10 3784 PMID: 31439839
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: 26148352
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
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? Please let us know.
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H1152 for spiral ganglion neuron differentiation.
By
Minjin Jeong on 08/09/2019
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: iPSCs
H1152 is used for spiral ganglion neuron differentiation.
H1152 is slightly better than Y27632 for neuronal differentiation.
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