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GNF4877
CAS No. 2041073-22-5
GNF4877( —— )
Catalog No. M23913 CAS No. 2041073-22-5
GNF4877 is a potent DYRK1A and GSK3β inhibitor (IC50s: 6 nM and 16 nM).
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 5MG | 123 | In Stock |
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| 10MG | 188 | In Stock |
|
| 25MG | 353 | In Stock |
|
| 50MG | 554 | In Stock |
|
| 100MG | 788 | In Stock |
|
| 200MG | 1051 | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameGNF4877
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NoteResearch use only, not for human use.
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Brief DescriptionGNF4877 is a potent DYRK1A and GSK3β inhibitor (IC50s: 6 nM and 16 nM).
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DescriptionGNF4877 is a potent DYRK1A and GSK3β inhibitor (IC50s: 6 nM and 16 nM). It leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation cells.
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In VitroHigh glucose concentrations and glucokinase activators (GKAs) increase Ca2+ signalling in β-cells, and increase intracellular Ca2+ leads to activation of calcineurin and nuclear translocation of NFATc proteins. Indeed, concentrations of GNF4877 ((0.1?μM, 0.3?μM) well below the EC50 for β-cell proliferation are able to induce proliferation in the presence of high glucose or pharmacological activators of glucokinase. Finally, increasing intracellular Ca2+ with glibenclamide (a sulfonylurea receptor 1 inhibitor) or Bay K8644 (an L-type Ca2+ channel activator) show additive activity with GNF4877.
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In VivoGNF4877 (50 mg/kg; oral gavage; twice a day; for 15 days; double transgenic RIP-DTA male mice) treatment induces β-cell proliferation, increases β-cell mass and insulin content, and improves glycaemic control. Animal Model:Double transgenic RIP-DTA male mice (Tg (Ins 2-rtTA) 2 Efr Tg (teto-DTA) 1 Gfi/J) with Doxycycline (28.8±2.4?g; 82±2 days) Dosage:50 mg/kg Administration:Oral gavage; twice a day; for 15 days Result:Induced β-cell proliferation, increased β-cell mass and insulin content, and improved glycaemic control.
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Synonyms——
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PathwayOthers
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TargetOther Targets
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RecptorGSK3β|DYRK1A
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Research Area——
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Indication——
Chemical Information
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CAS Number2041073-22-5
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Formula Weight494.52
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Molecular FormulaC25H27FN6O4
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Purity>98% (HPLC)
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SolubilityDMSO:4.17 mg/mL (8.43 mM; Need ultrasonic and warming)
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SMILESCC(C)OC1=CC(=C(C=C1)F)C2=CN=C(C(=N2)C(=O)NC3=C(C=CN=C3)N4CCC[C@H](C4)C(=O)O)N
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1.Shen W, et al. Inhibition of DYRK1A and GSK3β induces human β-cell proliferation. Nat Commun. 2015 Oct 26;6:8372.
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