H-1152 dihydrochloride
Based on 5 publication(s) in Google Scholar
H-1152 dihydrochloride is a membrane-permeable and selective ROCK inhibitor, with a Ki value of 1.6 nM, and an IC50 value of 12 nM for ROCK2.
For research use only. We do not sell to patients.
- Purity: 99.47%
- CAS No.: 871543-07-6
- Formula: C16H23Cl2N3O2S
- Molecular Weight:392.34
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) H-1152 dihydrochloride
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Biological Activity
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ROCKII 12 nM (IC50) |
CaMKII 0.18 μM (IC50) |
PKG 0.36 μM (IC50) |
AuroraA 0.745 μM (IC50) |
PKA 3.03 μM (IC50) |
Src 3.06 μM (IC50) |
PKC 5.68 μM (IC50) |
Abl 7.77 μM (IC50) |
MKK4 16.9 μM (IC50) |
MLCK 28.3 μM (IC50) |
EGFR 50 μM (IC50) |
GSK3α 60.7 μM (IC50) |
AMPK 100 μM (IC50) |
P38α 100 μM (IC50) |
H-1152 dihydrochloride is an inhibitor of Rho-kinase, with an IC50 of 12 nM for ROCK2. H-1152 (H-1152P) also shows less inhibitory activities against CaMKII, PKG, AuroraA, PKA, Src, PKC, MLCK, Abl, EGFR, MKK4, GSK3α, AMPK, and P38α, with IC50s of 0.180, 0.360, 0.745, 3.03, 3.06, 5.68, 28.3, 7.77, 50.0, 16.9, 60.7, 100, and 100 μM, respectively[1].
H-1152 potently inhibits Rho kinase, with a Ki of 1.6 nM, and slightly suppresses PKA, PKC and MLCK, with Kis of 0.63, 9.27, and 10.1 μM, respectively. H-1152 (0.1-10 μM) highly inhibits MARCKS phosphorylation, with an IC50 value of 2.5 μM in LPA-treated cells, but shows no such obvious effects in PDBu-treated cells[2].
H-1152 (0.5-10 μM) cuases no decreased neuronal survival. H-1152 (1, 5 or 10 μM) also exerts no alterations in the ratios of different neuronal morphologies. Furthermore, H-1152 (10 μM) increases neurite length in both BMP4 and LIF cultures[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 871543-07-6
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Appearance Solid
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Molecular Weight 392.34
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Formula C16H23Cl2N3O2S
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Color White to yellow
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SMILES
CC1=CN=CC2=C1C(S(=O)(N3[C@@H](C)CNCCC3)=O)=CC=C2.[H]Cl.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications (5)
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Journal Impact Factor
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Most Recent
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Acta Neuropathol Commun
Evaluation of Rho kinase inhibitor effects on neuroprotection and neuroinflammation in an ex-vivo retinal explant model. [Abstract]2024 Sep 14;12(1):150. PMID: 39300576 -
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Solvent & Solubility
H2O : 35.71 mg/mL (91.02 mM; Need ultrasonic)
DMSO : 10 mg/mL (25.49 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (2.55 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (2.55 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (127.44 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocol
Inhibitors (including H-1152) are added at the indicated concentrations to 50 µL of the assay mixture 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 1 mM dithiothreitol, 40 µM S6-peptide, various concentrations of [γ-32P]ATP and purified Rho-kinase. The reactions are started by the addition of [γ-32P]ATP and carried out at 30°C for 5 min. The Michaelis-Menten equation is used to calculate the Michaelis constant (Km) and maximal velocity (Vmax) of Rho-kinase. Data are further analyzed with secondary plot to calculate the inhibitory constant (Ki)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Briefly, cells are routinely plated on poly-d-lysine/laminin coated 96 well plates or in 16 well glass culture slides. Control medium contained Dulbecco's modified Eagles medium/Hams F12(1:1) (DMEM/F12), 2 mM l-glutamine, N2 mix (1:100 dilution), 0.63 mL of 45% glucose for each 100 mL of DMEM/F12, neurotrophin 3 (NT3; final concentration, 8 ng/mL), BDNF (final concentration 8 ng/mL), and 10% fetal bovine serum heat inactivated before use. LIF cultures contain control medium+LIF (50 ng/mL). BMP4 cultures contain control medium+bone morphogenetic protein 4 (BMP4; 25 ng/mL). Total volume of culture is 110 μL. ROCK inhibitor H-1152 is diluted in water and added in an additional 10 μL to cultures 24 h after plating. Water is added to controls. Eighteen hours after the addition of inhibitor, cultures are fixed in 4% paraformaldehyde (1 h at room temperature for peroxidase-linked labeling and 20 min at room temperature for fluorescence labeling). For ArrayScan/Cellomics automated analysis: Cells are plated in a total volume of 50 μL on 384 well plastic plates previously coated with poly-d-lysine/laminin, and cultured in the same medium[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (288 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Tamura M, et al. Development of specific Rho-kinase inhibitors and their clinical application. Biochim Biophys Acta. 2005 Dec 30;1754(1-2):245-52. Epub 2005 Sep 12. [Content Brief]
[2]. Ikenoya M, et al. Inhibition of rho-kinase-induced myristoylated alanine-rich C kinase substrate (MARCKS) phosphorylation in human neuronal cells by H-1152, a novel and specific Rho-kinase inhibitor. J Neurochem. 2002 Apr;81(1):9-16. [Content Brief]
[3]. Lie M, et al. Accelerated neurite growth from spiral ganglion neurons exposed to the Rho kinase inhibitor H-1152. Neuroscience. 2010 Aug 25;169(2):855-62. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 2.5488 mL | 12.7440 mL | 25.4881 mL | 63.7202 mL |
| 5 mM | 0.5098 mL | 2.5488 mL | 5.0976 mL | 12.7440 mL | |
| 10 mM | 0.2549 mL | 1.2744 mL | 2.5488 mL | 6.3720 mL | |
| 15 mM | 0.1699 mL | 0.8496 mL | 1.6992 mL | 4.2480 mL | |
| 20 mM | 0.1274 mL | 0.6372 mL | 1.2744 mL | 3.1860 mL | |
| 25 mM | 0.1020 mL | 0.5098 mL | 1.0195 mL | 2.5488 mL | |
| H2O | 30 mM | 0.0850 mL | 0.4248 mL | 0.8496 mL | 2.1240 mL |
| 40 mM | 0.0637 mL | 0.3186 mL | 0.6372 mL | 1.5930 mL | |
| 50 mM | 0.0510 mL | 0.2549 mL | 0.5098 mL | 1.2744 mL | |
| 60 mM | 0.0425 mL | 0.2124 mL | 0.4248 mL | 1.0620 mL | |
| 80 mM | 0.0319 mL | 0.1593 mL | 0.3186 mL | 0.7965 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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