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GSK-114
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Catalog No. T22341Cas No. 1301761-96-5
GSK-114 is a selective inhibitor of TNNI3 interacting kinase (TNNI3K) with an IC50 of 25 nM, 40-fold significant bias for TNNI3K compared to B-Raf with an IC50 of 1000 nM, so GSK-114 has excellent Broad-spectrum kinase selectivity and sufficient oral exposure enable use in cellular and in vivo studies.
GSK-114
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Purity: 99.51%
Catalog No. T22341Cas No. 1301761-96-5
GSK-114 is a selective inhibitor of TNNI3 interacting kinase (TNNI3K) with an IC50 of 25 nM, 40-fold significant bias for TNNI3K compared to B-Raf with an IC50 of 1000 nM, so GSK-114 has excellent Broad-spectrum kinase selectivity and sufficient oral exposure enable use in cellular and in vivo studies.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $34 | In Stock | In Stock | |
| 5 mg | $77 | In Stock | In Stock | |
| 10 mg | $127 | In Stock | In Stock | |
| 25 mg | $259 | In Stock | In Stock | |
| 50 mg | $413 | In Stock | In Stock | |
| 100 mg | $662 | In Stock | 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:99.51%
Appearance:Solid
Color:White
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Product Introduction
GSK-114 AI Summary
GSK-114 is a potent inhibitor of human TNNI3K, with an IC50 value of 25.0 nM as determined by fluorescence polarization assay. It also exhibits inhibitory activity against B-Raf, with an IC50 of 1000.0 nM, showing a selectivity index of 40.0 for TNNI3K over B-Raf. The compound's inhibition of myc-TNNI3K has an IC50 of 100.0 nM. In rat studies, GSK-114 demonstrated an AUC/dose value of 0.18 hr.Kg/L when administered orally.
The compound impacts cell viability differently across various cell types. In HEK293T cells, it generally promotes growth, with assay results ranging from 0.17 to 0.92. In U2OS cells, it also shows a positive effect on growth rates, albeit slightly lower, ranging from 0.39 to 0.84. In human fibroblast cells, the effects are mixed, with growth rates spanning from 0.29 to 0.69.
Regarding thermal stability, GSK-114 shows diverse effects across different protein domains. Notable changes include: an increase of 0.23°C at domain M1-K294, a decrease of 0.02°C at domain M1-L298, an increase of 0.24°C at domain M1-S360, a significant increase of 3.42°C at domain S229-K512, and a decrease of 3.63°C at domain N44-E168. Overall, GSK-114 exhibits both stabilizing and destabilizing effects on protein thermal stability depending on the specific domain..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | GSK-114 is a selective inhibitor of TNNI3 interacting kinase (TNNI3K) with an IC50 of 25 nM, 40-fold significant bias for TNNI3K compared to B-Raf with an IC50 of 1000 nM, so GSK-114 has excellent Broad-spectrum kinase selectivity and sufficient oral exposure enable use in cellular and in vivo studies. |
| Targets&IC50 | TNNI3K:25 nM |
| Molecular Weight | 417.48 |
| Formula | C19H23N5O4S |
| Cas No. | 1301761-96-5 |
| Smiles | CNS(=O)(=O)c1ccc(N(C)C)c(Nc2ncnc3cc(OC)c(OC)cc23)c1 |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 5.5 mg/mL (13.17 mM), Sonication is recommended.  | ||||||||||||||||||||
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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