GNF2133
Based on 1 publication(s) in Google Scholar
GNF2133 is a potent, selective and orally active DYRK1A inhibitor with IC50s of 0.0062, >50 µM for DYRK1A and GSK3β, respectively. GNF2133 shows good proliferation potency and efficacy on rat and human primary β-cell. GNF2133 significantly improves glucose disposal capacity and increases insulin secretion. GNF2133 has the potential for the research of type 1 diabetes.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.67%
- No. CAS: 2561414-56-8
- Fòrmula: C24H30N6O2
- Peso molecular:434.53
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) GNF2133
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Cell Proliferation/Viability Assay
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Flow Cytometry
Actividad biológica
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DYRK1A 0.0062 μM (IC50) |
GSK3β >50 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
>30 μM
Compound: 13g; GNF2133
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Displacement of [3H]dofetilide from human ERG expressed in CHO cells incubated for 90 mins by microbeta scintillation counting method
Displacement of [3H]dofetilide from human ERG expressed in CHO cells incubated for 90 mins by microbeta scintillation counting method
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[PMID: 32077280] |
| Pancreatic beta cell | EC50 |
0.21 μM
Compound: 13g; GNF2133
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Induction of cell proliferation in human beta cells incubated for 96 hrs by EdU incorporation assay
Induction of cell proliferation in human beta cells incubated for 96 hrs by EdU incorporation assay
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[PMID: 32077280] |
| Pancreatic beta cell | EC50 |
0.4 μM
Compound: 13g; GNF2133
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Induction of cell proliferation in rat beta cells incubated for 96 hrs by EdU incorporation assay
Induction of cell proliferation in rat beta cells incubated for 96 hrs by EdU incorporation assay
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[PMID: 32077280] |
| Sf21 | IC50 |
0.0062 μM
Compound: 13g; GNF2133
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Inhibition of recombinant human N-terminal GST-tagged DYRK1A (1 to 763 residues) expressed in Sf21 cells using Ulight-glycogen synthase as substrate incubated for 60 mins by TR-FRET LANCE method
Inhibition of recombinant human N-terminal GST-tagged DYRK1A (1 to 763 residues) expressed in Sf21 cells using Ulight-glycogen synthase as substrate incubated for 60 mins by TR-FRET LANCE method
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[PMID: 32077280] |
| Sf9 | IC50 |
>50 μM
Compound: 13g; GNF2133
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Inhibition of recombinant human His/GST-tagged GSK3beta (2 to 433 residues) expressed in baculovirus infected Sf9 cells using Ulight-glycogen synthase peptide as substrate incubated for 30 mins by TR-FRET LANCE method
Inhibition of recombinant human His/GST-tagged GSK3beta (2 to 433 residues) expressed in baculovirus infected Sf9 cells using Ulight-glycogen synthase peptide as substrate incubated for 30 mins by TR-FRET LANCE method
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[PMID: 32077280] |
GNF2133 (30 mg/kg; p.o.; once a day for 5 days) shows the ability to proliferate β-cells in vivo[1].
GNF2133 (3, 10, 30 mg/kg) significantly improves glucose disposal capacity and increased insulin secretion in RIP-DTA mice[1].
Pharmacokinetic Parameters of GNF2133 in CD-1 mice[1].
| plasma (iv) | plasma (po) | pancreas (po) | |
| CL (mL/min/kg) | 23.5 | / | / |
| Vss (L/kg) | 11 | / | / |
| AUC (h·nM) | 3268 | 10974 | 144420 |
| Cmax(nM) | 1977 | 1675 | 13319 |
| tmax<(h) | 0.03 | 3.0 | 3.0 |
| Clast(nM) | 36.6 | 19 | 1324 |
| t1/2<(h) | 6.6 | 3.4 | 6.6 |
| F (%) | / | 22.3 | / |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-1 mice[1]
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Dosage:30 mg/kg
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Administration:P.o.
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Result:Showed good oral absorption and moderate plasma exposure with oral bioavailability of 22.3%.
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Animal Model:Wistar Han rat[1]
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Dosage:30 mg/kg (0.5% methylcellulose + Tween-80)
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Administration:P.o.; once a day for 5 days
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Result:Increased cyclin D1 levels and overall cell density, and increased in cell proliferation marker Ki67 and insulin.
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Animal Model:Diphtheria toxin A (RIP-DTA) mice[1]
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Dosage:3, 10, 30 mg/kg (20 mg/kg doxycycline (Dox) for 5 days)
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Administration:P.o., once a day for 35 days
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Result:Significantly improves glucose disposal capacity and increased insulin secretion.
Chemical Information
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No. CAS 2561414-56-8
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Appearance Solid
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Peso molecular 434.53
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Fòrmula C24H30N6O2
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Color Off-white to pink
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SMILES
CCN1CCN(CC1)C(NC2=NC=CC(C3=CN(C4=CN=CC=C34)C5CCOCC5)=C2)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Genet
Chromothripsis-associated chromosome 21 amplification orchestrates transformation to blast-phase MPN through targetable overexpression of DYRK1A. [Abstract]2025 Jun;57(6):1478-1492. PMID: 40490510
GNF2133 purchased from MedChemExpress. Usage Cited in: Nat Genet. 2025 Jun;57(6):1478-1492. [Abstract]
Dose-dependent reduction of HEL cell proliferation in culture with the DYRK1A inhibitor GNF2133 (0.01, 0.1, 5, 10 μM).
GNF2133 purchased from MedChemExpress. Usage Cited in: Nat Genet. 2025 Jun;57(6):1478-1492. [Abstract]
Representative flow cytometry plots for Annexin V PI apoptosis assay demonstrating synergy between the DYRK1A inhibitor GNF2133 (‘GNF”) (100 nM) and the BCL2/BCL-XL inhibitor navitoclax (“NAV”).
Solvente y solubilidad
DMSO : 5 mg/mL (11.51 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 0.5 mg/mL (1.15 mM); Clear solution
This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.5 mg/mL (1.15 mM); Clear solution
This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Pureza y Documentación
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Ficha de datos (281 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3013 mL | 11.5067 mL | 23.0134 mL | 57.5334 mL |
| 5 mM | 0.4603 mL | 2.3013 mL | 4.6027 mL | 11.5067 mL | |
| 10 mM | 0.2301 mL | 1.1507 mL | 2.3013 mL | 5.7533 mL |
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