RKI-1447
Based on 4 publication(s) in Google Scholar
RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2 with IC50 values of 14.5 nM and 6.2 nM, respectively.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.02%
- CAS. Nr.: 1342278-01-6
- Formel: C16H14N4O2S
- Molecular Weight:326.37
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Publications Citing Use of MedChemExpress (MCE) RKI-1447
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Biologische Aktivität
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ROCK2 6.2 nM (IC50) |
ROCK1 14.5 nM (IC50) |
RKI-1447 is a Type I kinase inhibitor that binds the ATP binding site through interactions with the hinge region and the DFG motif. RKI-1447 suppresses phosphorylation of the ROCK substrates mLC-2 and MYPT-1 in human cancer cells, but has no effect on the phosphorylation levels of the AKT, MEK and S6 kinase at concentrations as high as 10 μM. RKI-1447 is also highly selective at inhibiting ROCK-mediated cytoskeleton re-organization. RKI-1447 inhibits migration, invasion and anchorage-independent tumor growth of breast cancer cells[1].
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.
Chemical Information
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CAS. Nr. 1342278-01-6
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Appearance Solid
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Molecular Weight 326.37
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Formel C16H14N4O2S
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Color White to off-white
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SMILES
O=C(NC1=NC(C2=CC=NC=C2)=CS1)NCC3=CC=CC(O)=C3
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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 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Int J Mol Sci
A Functional Pipeline of Genome-Wide Association Data Leads to Midostaurin as a Repurposed Drug for Alzheimer's Disease. [Abstract]2023 Jul 28;24(15):12079. PMID: 37569459 -
Cell Signal
ROCK1 drives colorectal cancer liver metastasis via PRKCH-mediated bioenergetic reprogramming. [Abstract]2025 Oct 18:112174. PMID: 41115563 -
Virology
2024 Dec:600:110233. PMID: 39255726 -
Med Sci Monit
The Effects of RKI-1447 in a Mouse Model of Nonalcoholic Fatty Liver Disease Induced by a High-Fat Diet and in HepG2 Human Hepatocellular Carcinoma Cells Treated with Oleic Acid. [Abstract]2020 Feb 6:26:e919220. PMID: 32026851
RKI-1447 purchased from MedChemExpress. Usage Cited in: Med Sci Monit. 2020 Feb 6:26:e919220. [Abstract]
The effects of RKI-1447 on glucose tolerance and insulin resistance in a mouse model of nonalcoholic fatty liver disease (NAFLD) induced by a high-fat diet. The expression of the insulin receptor substrate-1 (IRS1) are shown. The mice were fed with a high-fat diet for 12 weeks. From the ninth week, the mice were treated orally with the ROCK inhibitor RKI-1447 (2 mg/kg to 8 mg/kg) twice weekly for three weeks.
Lösungsmittel & Löslichkeit
DMSO : ≥ 50 mg/mL (153.20 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
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 (7.66 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
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
Compounds are tested on three separate days with 8 point dilutions performed in duplicate to determine average IC50 values. The assay conditions are optimized to 15 µL of kinase reaction volume with 5 ng of enzyme in 50 mM HEPES (pH 7.5), 10 mM MgCl2, 1 mM EGTA, and 0.01% Brij-35. The reaction is incubated for 1 h at room temperature in the presence of 1.5 µM of peptide substrate with 12.5 µM of ATP (for ROCK1) or 2 µM of substrate with 50 µM of ATP (for ROCK2). The reaction is then stopped and the ratio of phosphorylated to unphosphorylated peptides is determined by selective cleavage of only the unphosphorylated peptide. The ratio of the signals at 445 nm and 520 nm is measured. IC50 values are determined using fitted curves with GraphPad Prism 5 software[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
NIH 3T3 cells are plated at 8000 cells/well in 8-chamber slides in serum free media for 24 hours, and treated with vehicle, 1 μM RKI-1447 or 1 μM RKI-1313 for 1 hour. The cells are then stimulated with complete media, 10 μM LPA, 200 ng/mL bradykinin or 30 ng/mL PDGF for 30 mins. After stimulation, the cells are fixed in 4% paraformaldehyde and stained with Texas-Red Phalloidin. Mounting medium containing DAPI is then added and at least 100 cells per well are observed[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: MMTV/neu transgenic mice are treated i.p. daily for 14 days with either Vehicle [20%-2-hydroxypropyl-beta-cyclodextrin (HPCD)] or 200 mpk RKI-1447 dissolved in freshly prepared HPCD. The percent change in volume is calculated on the basis of the tumor volume on the last day of treatment (Vf) relative to that on the day of initiation of treatment (V0). The average percent change in tumor volume is then calculated for each treatment group[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
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 | 3.0640 mL | 15.3200 mL | 30.6401 mL | 76.6002 mL |
| 5 mM | 0.6128 mL | 3.0640 mL | 6.1280 mL | 15.3200 mL | |
| 10 mM | 0.3064 mL | 1.5320 mL | 3.0640 mL | 7.6600 mL | |
| 15 mM | 0.2043 mL | 1.0213 mL | 2.0427 mL | 5.1067 mL | |
| 20 mM | 0.1532 mL | 0.7660 mL | 1.5320 mL | 3.8300 mL | |
| 25 mM | 0.1226 mL | 0.6128 mL | 1.2256 mL | 3.0640 mL | |
| 30 mM | 0.1021 mL | 0.5107 mL | 1.0213 mL | 2.5533 mL | |
| 40 mM | 0.0766 mL | 0.3830 mL | 0.7660 mL | 1.9150 mL | |
| 50 mM | 0.0613 mL | 0.3064 mL | 0.6128 mL | 1.5320 mL | |
| 60 mM | 0.0511 mL | 0.2553 mL | 0.5107 mL | 1.2767 mL | |
| 80 mM | 0.0383 mL | 0.1915 mL | 0.3830 mL | 0.9575 mL | |
| 100 mM | 0.0306 mL | 0.1532 mL | 0.3064 mL | 0.7660 mL |
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