ROCK inhibitor-2 |
Catalog No.GC37551
One-Click Copy Product Info
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ROCK inhibitor-2 is a selective Rho kinase (ROCK) inhibitor with IC50 values of 17nM and 2nM for ROCK1 and ROCK2, respectively, and has anti-tumor activity.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1127308-52-4
Sample solution is provided at 25 µL, 10mM.
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ROCK inhibitor-2 is a selective Rho kinase (ROCK) inhibitor with IC50 values of 17nM and 2nM for ROCK1 and ROCK2, respectively, and has anti-tumor activity[1, 2]. ROCK is a serine/threonine protein kinase and a downstream target effector molecule of Rho. ROCK can regulate multiple functions such as cell contraction, migration, adhesion and proliferation[3, 4]. ROCK inhibitor-2 belongs to the aminopyridine class of compounds and is a structural analog of Y-27632[5]. ROCK inhibitor-2 may help improve vision loss and treat glaucoma[6].
In vitro, treatment of human osteosarcoma cell line (U2OS cells) with ROCK inhibitor-2 (50μM) for 48h significantly inhibited cell migration and invasion and caused mitochondrial dysfunction[2].
References:
[1]Feng Y, LoGrasso P V, Defert O, et al. Rho kinase (ROCK) inhibitors and their therapeutic potential[J]. Journal of medicinal chemistry, 2016, 59(6): 2269-2300.
[1] Zhang W, Zhao W, Li Q, et al. 3D-printing magnesium–polycaprolactone loaded with melatonin inhibits the development of osteosarcoma by regulating cell-in-cell structures[J]. Journal of Nanobiotechnology, 2021, 19: 1-20.
[3]Liu J, Wada Y, Katsura M, et al. Rho-associated coiled-coil kinase (ROCK) in molecular regulation of angiogenesis[J]. Theranostics, 2018, 8(21): 6053.
[4]Liao J K, Seto M, Noma K. Rho kinase (ROCK) inhibitors[J]. Journal of cardiovascular pharmacology, 2007, 50(1): 17-24.
[5]Shahin R, Shaheen O, El-Dahiyat F, et al. Research advances in kinase enzymes and inhibitors for cardiovascular disease treatment[J]. Future science OA, 2017, 3(4): FSO204.
[6]Abbhi V, Piplani P. Rho-kinase (ROCK) inhibitors-a neuroprotective therapeutic paradigm with a focus on ocular utility[J]. Current Medicinal Chemistry, 2020, 27(14): 2222-2256.
| Cell experiment [1]: | |
Cell lines | U2OS cells |
Preparation Method | U2OS cells were seeded in 6-well plates at a density of 8.5×105/well, and 1mM melatonin and 50µM ROCK inhibitor-2 were added. After 48h of culture, the cells were scratched with a pipette tip. Subsequently, they were incubated with DMEM medium containing 0.5% FBS. After repeated treatment at 0, 12, 24, and 48h, cell photos were taken using a phase contrast microscope. |
Reaction Conditions | 50μM; 48h |
Applications | ROCK inhibitor-2 treatment significantly reduced the cell migration area. |
References: | |
| Cas No. | 1127308-52-4 | SDF | |
| Canonical SMILES | O=C(N[C@H](C)C1=CC=CC(OC)=C1)C(C=C2)=CC=C2C3=CC=NC=C3 | ||
| Formula | C21H20N2O2 | M.Wt | 332.4 |
| Solubility | DMSO: 250 mg/mL (752.11 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.0084 mL | 15.0421 mL | 30.0842 mL |
| 5 mM | 601.7 μL | 3.0084 mL | 6.0168 mL |
| 10 mM | 300.8 μL | 1.5042 mL | 3.0084 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)