GNF2133 (hydrochloride)

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[1].

Product Specifications

CAS Number

[2561414-57-9]

UNSPSC

12352005

Target

DYRK

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/gnf2133-hydrochloride.html

Purity

99.86

Solubility

DMSO : 4 mg/mL (ultrasonic; warming; heat to 60°C) |H2O : 100 mg/mL (ultrasonic)

Smiles

O=C(N1CCN(CC1)CC)NC2=NC=CC(C3=CN(C4CCOCC4)C5=C3C=CN=C5)=C2.Cl

Molecular Formula

C24H31ClN6O2

Molecular Weight

470.99

References & Citations

[1]Liu YA, et al. Selective DYRK1A Inhibitor for the Treatment of Type 1 Diabetes: Discovery of 6-Azaindole Derivative GNF2133. J Med Chem. 2020 Mar 26;63 (6) :2958-2973.