ROCK inhibitor-2
Based on 2 publication(s) in Google Scholar
ROCK inhibitor-2 (compound 6) is a selective dual inhibitor of ROCK1 and ROCK2, with IC50 values of 160 nM and 21 nM, respectively. ROCK inhibitor-2 inhibits pMYPT1 with IC50 of 75 nM. ROCK inhibitor-2 exhibits antitumor activity.
For research use only. We do not sell to patients.
- Purity: 99.92%
- CAS No.: 1127308-52-4
- Formula: C21H20N2O2
- Molecular Weight:332.40
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) ROCK inhibitor-2
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Biological Activity
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ROCK1 160 nM (IC50) |
ROCK2 21 nM (IC50) |
ROCK inhibitor-2 (50 μM, 24-48 h) reduces the formation of cell-in-cell structure in cell U2OS, inhibits the cell migration and invasion of U2OS, and leads to mitochondrial dysfunction[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:U2OS xenograft mouse models[2]
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Dosage:10 mg/kg*day
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Administration:ip, 27 days
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Result:Inhibited tumor growth.
Chemical Information
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CAS No. 1127308-52-4
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Appearance Solid
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Molecular Weight 332.40
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Formula C21H20N2O2
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Color White to light yellow
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SMILES
O=C(N[C@H](C)C1=CC=CC(OC)=C1)C(C=C2)=CC=C2C3=CC=NC=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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J Nanobiotechnology
3D-printing magnesium-polycaprolactone loaded with melatonin inhibits the development of osteosarcoma by regulating cell-in-cell structures. [Abstract]2021 Sep 4;19(1):263. PMID: 34481503 -
Solvent & Solubility
DMSO : 200 mg/mL (601.68 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 5 mg/mL (15.04 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (15.04 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (251 KB)
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- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Hobson AD, et al. Identification of Selective Dual ROCK1 and ROCK2 Inhibitors Using Structure-Based DrugDesign. J Med Chem. 2018 Dec 27;61(24):11074-11100. [Content Brief]
[2]. Zhang W, et al., 3D-printing magnesium-polycaprolactone loaded with melatonin inhibits the development of osteosarcoma by regulating cell-in-cell structures. J Nanobiotechnology. 2021 Sep 4;19(1):263. [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. 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 | 1 mM | 3.0084 mL | 15.0421 mL | 30.0842 mL | 75.2106 mL |
| 5 mM | 0.6017 mL | 3.0084 mL | 6.0168 mL | 15.0421 mL | |
| 10 mM | 0.3008 mL | 1.5042 mL | 3.0084 mL | 7.5211 mL | |
| 15 mM | 0.2006 mL | 1.0028 mL | 2.0056 mL | 5.0140 mL | |
| 20 mM | 0.1504 mL | 0.7521 mL | 1.5042 mL | 3.7605 mL | |
| 25 mM | 0.1203 mL | 0.6017 mL | 1.2034 mL | 3.0084 mL | |
| 30 mM | 0.1003 mL | 0.5014 mL | 1.0028 mL | 2.5070 mL | |
| 40 mM | 0.0752 mL | 0.3761 mL | 0.7521 mL | 1.8803 mL | |
| 50 mM | 0.0602 mL | 0.3008 mL | 0.6017 mL | 1.5042 mL | |
| 60 mM | 0.0501 mL | 0.2507 mL | 0.5014 mL | 1.2535 mL | |
| 80 mM | 0.0376 mL | 0.1880 mL | 0.3761 mL | 0.9401 mL | |
| 100 mM | 0.0301 mL | 0.1504 mL | 0.3008 mL | 0.7521 mL |
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