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GSK-25
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Catalog No. T4488Cas No. 874119-56-9
Alias GSK25
GSK-25 maintains good selectivity against a panel of 31 kinases, as well as RSK1 and p70S6K (RSK1 IC50 of 398 nM, p70S6K IC50 of 1000nM), and a dramatically improved P450 profile (>2.2 uM at all isozymes tested).
GSK-25
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Purity: 99.29%
Catalog No. T4488Alias GSK25Cas No. 874119-56-9
GSK-25 maintains good selectivity against a panel of 31 kinases, as well as RSK1 and p70S6K (RSK1 IC50 of 398 nM, p70S6K IC50 of 1000nM), and a dramatically improved P450 profile (>2.2 uM at all isozymes tested).
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $39 | In Stock | In Stock | |
| 2 mg | $54 | In Stock | In Stock | |
| 5 mg | $84 | In Stock | In Stock | |
| 10 mg | $119 | In Stock | In Stock | |
| 25 mg | $180 | In Stock | In Stock | |
| 50 mg | $286 | In Stock | In Stock | |
| 100 mg | $478 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $96 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Batch Information
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Purity:99.29%
Appearance:Solid
Color:Yellow
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Product Introduction
GSK-25 AI Summary
GSK-25 exhibits substantial bioactivity, including potent inhibition of human recombinant ROCK1 kinase with an IC50 value of 6.0 nM. It shows moderate inhibition of CYP2C9, CYP2D6, and CYP3A4 enzymes with IC50 values of 2500.0 nM and 5200.0 nM, respectively. Additionally, 513871 efficiently inhibits phenylephrine-induced aortic ring contraction in Sprague-Dawley rats with an IC50 of 256.0 nM and reduces mean arterial pressure by 25.0 mmHg in an anesthetized spontaneous hypertensive rat model at a dose of 30 mg/kg.
The compound also demonstrates moderate inhibition of p70S6K and RSK1, with IC50 values of 1000.0 nM and 398.0 nM, respectively. Pharmacokinetic evaluations reveal favorable properties, including a half-life of 105.0 hours in Sprague-Dawley rats and 2.2 hours in monkeys, with moderate to high oral bioavailability (49.0% in rats and 19.0% in monkeys) and moderate clearance and volume of distribution in rats (36.0 mL.min-1.kg-1 and 2.0 L.kg-1).
In a PubChem BioAssay qHTS profiling assay, GSK-25 shows a potency of 21117.7 nM against Plasmodium falciparum (DD2) proliferation..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | GSK-25 maintains good selectivity against a panel of 31 kinases, as well as RSK1 and p70S6K (RSK1 IC50 of 398 nM, p70S6K IC50 of 1000nM), and a dramatically improved P450 profile (>2.2 uM at all isozymes tested). |
| Targets&IC50 | mTOR (p70S6K):1000nM, RSK1:398 nM, ROCK1:7 nM |
| Synonyms | GSK25 |
| Molecular Weight | 513.33 |
| Formula | C24H16Cl2F2N6O |
| Cas No. | 874119-56-9 |
| Smiles | CC1=C(C(N=C(N1)c1ccnc(Cl)c1)c1ccc(Cl)cc1F)C(=O)Nc1cc2cn[nH]c2cc1F |
| Relative Density. | 1.57 g/cm3 (Predicted) |
| Storage | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 60 mg/mL (116.88 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.9 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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