GNF4877
GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6 nM and 16 nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66 μM for mouse β (R7T1) cells) [1].
Product Specifications
CAS Number
[2041073-22-5]
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
DYRK; GSK-3
Type
Reference compound
Related Pathways
PI3K/Akt/mTOR; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt
Applications
Metabolism-sugar/lipid metabolism
Field of Research
Metabolic Disease
Assay Protocol
https://www.medchemexpress.com/gnf4877.html
Purity
99.82
Solubility
DMSO : 3.33 mg/mL (ultrasonic; warming; heat to 60°C)
Smiles
O=C([C@H]1CN(C2=C(NC(C3=NC(C4=CC(OC(C)C)=CC=C4F)=CN=C3N)=O)C=NC=C2)CCC1)O
Molecular Formula
C25H27FN6O4
Molecular Weight
494.52
Precautions
H302, H315, H319, H335
References & Citations
[1]Shen W, et al. Inhibition of DYRK1A and GSK3β induces human β-cell proliferation. Nat Commun. 2015 Oct 26;6:8372.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
DYRK1; GSK-3β
Available Sizes
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