H-1152
Based on 5 publication(s) in Google Scholar
H-1152 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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.00%
- CAS. Nr.: 451462-58-1
- Formel: C16H21N3O2S
- Molecular Weight:319.42
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Publications Citing Use of MedChemExpress (MCE) H-1152
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Biologische Aktivität
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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) |
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Cell Line
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Type | Value | Description | References |
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| NT2 | IC50 |
2500 nM
Compound: K00003, H-1152
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Inhibition of lysophosphatidic acid-induced MARCKS phosphorylation in human NT2 cells
Inhibition of lysophosphatidic acid-induced MARCKS phosphorylation in human NT2 cells
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[PMID: 18077363] |
H-1152 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. Nr. 451462-58-1
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Appearance Solid
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Molecular Weight 319.42
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Formel C16H21N3O2S
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Color White to light yellow
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SMILES
CC1=CN=CC2=C1C(S(=O)(N3[C@@H](C)CNCCC3)=O)=CC=C2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
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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Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (313.07 mM; Need ultrasonic; 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: 2.5 mg/mL (7.83 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (7.83 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
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.
Reinheit & Dokumentation
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Data Sheet (285 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
Verweise
[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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1307 mL | 15.6534 mL | 31.3067 mL | 78.2669 mL |
| 5 mM | 0.6261 mL | 3.1307 mL | 6.2613 mL | 15.6534 mL | |
| 10 mM | 0.3131 mL | 1.5653 mL | 3.1307 mL | 7.8267 mL | |
| 15 mM | 0.2087 mL | 1.0436 mL | 2.0871 mL | 5.2178 mL | |
| 20 mM | 0.1565 mL | 0.7827 mL | 1.5653 mL | 3.9133 mL | |
| 25 mM | 0.1252 mL | 0.6261 mL | 1.2523 mL | 3.1307 mL | |
| 30 mM | 0.1044 mL | 0.5218 mL | 1.0436 mL | 2.6089 mL | |
| 40 mM | 0.0783 mL | 0.3913 mL | 0.7827 mL | 1.9567 mL | |
| 50 mM | 0.0626 mL | 0.3131 mL | 0.6261 mL | 1.5653 mL | |
| 60 mM | 0.0522 mL | 0.2609 mL | 0.5218 mL | 1.3044 mL | |
| 80 mM | 0.0391 mL | 0.1957 mL | 0.3913 mL | 0.9783 mL | |
| 100 mM | 0.0313 mL | 0.1565 mL | 0.3131 mL | 0.7827 mL |
H-1152 Related Classifications
HY-15720 Related Classifications
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