GNF2133 hydrochloride
Based on 1 publication(s) in Google Scholar
GNF2133 hydrochloride is a potent, selective and orally active DYRK1A inhibitor with IC50s of 0.0062, >50 µM for DYRK1A and GSK3β, respectively. GNF2133 hydrochloride shows good proliferation potency and efficacy on rat and human primary β-cell. GNF2133 hydrochloride significantly improves glucose disposal capacity and increases insulin secretion. GNF2133 hydrochloride has the potential for the research of type 1 diabetes.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.29%
- CAS 番号: 2561414-57-9
- 分子式: C24H31ClN6O2
- 分子量:470.99
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 GNF2133 hydrochloride
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Cell Proliferation/Viability Assay
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生物活性
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DYRK1A 0.0062 μM (IC50) |
GSK3β >50 μM (IC50) |
GNF2133 hydrochloride (30 mg/kg; p.o.; once a day for 5 days) shows the ability to proliferate β-cells in vivo[1].
GNF2133 hydrochloride (3, 10, 30 mg/kg) significantly improves glucose disposal capacity and increased insulin secretion in RIP-DTA mice[1].
Pharmacokinetic Parameters of GNF2133 hydrochloride 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.
化学情報
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CAS 番号 2561414-57-9
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性状 Solid
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分子量 470.99
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分子式 C24H31ClN6O2
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Color Off-white to light brown
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SMILES
O=C(N1CCN(CC1)CC)NC2=NC=CC(C3=CN(C4CCOCC4)C5=C3C=CN=C5)=C2.Cl
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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 hydrochloride 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 hydrochloride 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”).
溶剤 & 溶解度
H2O : 100 mg/mL (212.32 mM; Need ultrasonic)
DMSO : 4 mg/mL (8.49 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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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: ≥ 0.4 mg/mL (0.85 mM); Clear solution
This protocol yields a clear solution of ≥ 0.4 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (4.0 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: ≥ 0.4 mg/mL (0.85 mM); Clear solution
This protocol yields a clear solution of ≥ 0.4 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (4.0 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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
純度とドキュメンテーション
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データシート (282 KB)
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取扱説明書 (2659 KB)
参考文献
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 / H2O | 1 mM | 2.1232 mL | 10.6159 mL | 21.2319 mL | 53.0797 mL |
| 5 mM | 0.4246 mL | 2.1232 mL | 4.2464 mL | 10.6159 mL | |
| H2O | 10 mM | 0.2123 mL | 1.0616 mL | 2.1232 mL | 5.3080 mL |
| 15 mM | 0.1415 mL | 0.7077 mL | 1.4155 mL | 3.5386 mL | |
| 20 mM | 0.1062 mL | 0.5308 mL | 1.0616 mL | 2.6540 mL | |
| 25 mM | 0.0849 mL | 0.4246 mL | 0.8493 mL | 2.1232 mL | |
| 30 mM | 0.0708 mL | 0.3539 mL | 0.7077 mL | 1.7693 mL | |
| 40 mM | 0.0531 mL | 0.2654 mL | 0.5308 mL | 1.3270 mL | |
| 50 mM | 0.0425 mL | 0.2123 mL | 0.4246 mL | 1.0616 mL | |
| 60 mM | 0.0354 mL | 0.1769 mL | 0.3539 mL | 0.8847 mL | |
| 80 mM | 0.0265 mL | 0.1327 mL | 0.2654 mL | 0.6635 mL | |
| 100 mM | 0.0212 mL | 0.1062 mL | 0.2123 mL | 0.5308 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
GNF2133 hydrochloride 関連分類
HY-142295A 関連分類
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