GNF7156
GNF7156 is a DYRK1A/GSK3B inhibitor, IC50 values of 100 nM for DYRK1A and 40 nM for GSK3B. GNF7156 inhibits DYRK1A and GSK3B kinase activity and induces NFAT nuclear retention. GNF7156 stimulates beta-cell cycle entry and division and maintains insulin secretory capacity. GNF7156 can be used for the research of type 1 diabetes, and type 2 diabetes.
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- CAS No.: 2041071-54-7
- Formule: C22H22N6O3
- Masse moléculaire:418.45
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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GSK3β 40 nM (IC50) |
DYRK1A 100 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| Pancreatic beta cell | EC50 |
0.76 nM
Compound: 14; GNF7156
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Induction of human Pancreatic beta cell proliferation at 50 mg/kg measured after 5 days in presence of EdU incorporation by Cell-Titer Glo assay
Induction of human Pancreatic beta cell proliferation at 50 mg/kg measured after 5 days in presence of EdU incorporation by Cell-Titer Glo assay
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[PMID: 33682417] |
GNF7156 (4 days) potently stimulates proliferation of reversibly immortalized mouse beta (R7T1) cells with an EC50 of 2.2 μM[1].
GNF7156 (4 days) induces DNA synthesis in 15-30% of dissociated adult primary rat pancreatic β-cells[1].
GNF7156 (4 days) induces DNA synthesis in 3-6% of dissociated adult primary human pancreatic β-cells with an EC50 of 0.76 μM[1].
GNF7156 potently inhibits purified GSK3B enzyme activity with an IC50 of 40 nM[1].
GNF7156 induces β-catenin nuclear translocation in dispersed primary rat pancreatic β-cells, confirming cellular GSK3B inhibition[1].
GNF7156 (4 days)-induced proliferation of dispersed primary rat pancreatic β-cells is partially inhibited by overexpression of wild-type or constitutively active GSK3B, but not kinase-dead GSK3B[1].
GNF7156 potently inhibits purified DYRK1A enzyme activity with an IC50 of 100 nM[1].
GNF7156 (4 days)-induced proliferation of dispersed primary rat pancreatic β-cells is inhibited by overexpression of wild-type DYRK1A, but not kinase-dead DYRK1A[1].
GNF7156 (10 min-3 h) induces nuclear localization of NFATc1-GFP in INS1E rat insulinoma cells[1].
GNF7156 inhibits NFATc1 nuclear export in INS1E rat insulinoma cells, maintaining nuclear NFATc1 localization after calcium ionophore withdrawal[1].
GNF7156 (6.7 μM; 7 days) increases DNA content, ATP content, and islet equivalent units in intact primary human pancreatic islets while preserving glucose-stimulated insulin secretion, despite a slight reduction in total insulin content[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
GNF7156 significantly increases human β-cell proliferation in diabetic NOD-SCID mice transplanted with human islets[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2041071-54-7
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Masse moléculaire 418.45
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Formule C22H22N6O3
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SMILES
O=C(C1CCN(CC1)C2=C(NC(C3=C(N)N=CC(C4=CC=CC=C4)=N3)=O)C=NC=C2)O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Shen W, et al. Inhibition of DYRK1A and GSK3B induces human β-cell proliferation. Nat Commun. 2015 Oct 26;6:8372. [Content Brief]
[2]. Liu YA, et al. Selective DYRK1A Inhibitor for the Treatment of Type 1 Diabetes: Discovery of 6-Azaindole Derivative GNF2133. J Med Chem. 2020;63(6):2958-2973. [Content Brief]
[3]. Shirakawa J, et al. Novel factors modulating human β-cell proliferation. Diabetes Obes Metab. 2016;18 Suppl 1(Suppl 1):71-77. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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