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GNF2133 is an effective and selective inhibitor of DYRK1A with IC50s of 6.2 nM. GNF2133 can be used in studies about type 1 diabetes.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $132 | In Stock | In Stock | |
| 5 mg | $328 | In Stock | In Stock | |
| 10 mg | $496 | In Stock | In Stock | |
| 25 mg | $828 | In Stock | In Stock | |
| 50 mg | $1,230 | In Stock | In Stock | |
| 100 mg | $1,730 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $376 | In Stock | In Stock |
| Description | GNF2133 is an effective and selective inhibitor of DYRK1A with IC50s of 6.2 nM. GNF2133 can be used in studies about type 1 diabetes. |
| Targets&IC50 | DYRK1A:0.0062 μM, GSK-3β:>50 μM |
| In vitro | GNF2133 has an IC50 of >50 µM for GSK3β. GNF2133 significantly improves glucose disposal capacity and increases insulin secretion[1]. |
| In vivo | In Diphtheria toxin A (RIP-DTA) mice, GNF2133 (3, 10, 30 mg/kg) significantly improves glucose disposal capacity and increased insulin secretion. In CD-1 mice, GNF2133 (30 mg/kg; p.o.) shows moderate plasma exposure and good oral absorption with oral bioavailability of 22.3%[1]. In Wistar Han rat, GNF2133 (30 mg/kg; p.o.) increases in cell proliferation marker Ki67 and insulin and reduces cyclin D1 levels and overall cell density[1]. |
| Molecular Weight | 434.53 |
| Formula | C24H30N6O2 |
| Cas No. | 2561414-56-8 |
| Smiles | CCN1CCN(CC1)C(=O)Nc1cc(ccn1)-c1cn(C2CCOCC2)c2cnccc12 |
| 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: 4.5 mg/mL (10.36 mM), Sonication is recommended. | ||||||||||||||||||||
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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