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GSK-626616 is a potent and orally bioavailable DYRK3 inhibitor (IC50: 0.7 nM). It inhibits other members of the DYRK family with similar potency. GSK-626616 is a potential therapy for the treatment of anemia.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $44 | In Stock | In Stock | |
| 5 mg | $77 | In Stock | In Stock | |
| 10 mg | $139 | In Stock | In Stock | |
| 25 mg | $296 | In Stock | In Stock | |
| 50 mg | $546 | In Stock | In Stock | |
| 100 mg | $789 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $97 | In Stock | In Stock |
| Description | GSK-626616 is a potent and orally bioavailable DYRK3 inhibitor (IC50: 0.7 nM). It inhibits other members of the DYRK family with similar potency. GSK-626616 is a potential therapy for the treatment of anemia. |
| Targets&IC50 | β-glucuronidase:0.7 nM |
| In vitro | GSK-626616 (serum-deprived HeLa cells) reduces EGF-induced phosphorylation of PRAS40 at Thr246. GSK-626616 enhances the binding of PRAS40 to mTORC1[2]. GSK-626616 abolishes the phosphorylation of S6K1 at Thr389 in nonstimulated HeLa cells. GSK-626616 reduces the phosphorylation of S6K1 at Thr389 in EGF- and insulin-stimulated HeLa cells, showing that mTORC1 activity is impaired[2]. |
| Molecular Weight | 401.27 |
| Formula | C18H10Cl2N4OS |
| Cas No. | 1025821-33-3 |
| Smiles | Clc1cccc(Cl)c1NC1=NC(=O)\C(S1)=C\c1ccc2nccnc2c1 |
| Relative Density. | 1.55 g/cm3 (Predicted) |
| 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: 49 mg/mL (122.11 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (12.46 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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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.
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.
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