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GNF2133

GNF2133 is a potent, selective and orally active DYRK1A inhibitor with IC50s of 0.0062, >50 μM for DYRK1A and GSK3β, respectively. GNF2133 shows good proliferation potency and efficacy on rat and human primary β-cell. GNF2133 significantly improves glucose disposal capacity and increases insulin secretion. GNF2133 has the potential for the research of type 1 diabetes[1].

Product Specifications

CAS Number

[2561414-56-8]

UNSPSC

12352005

Hazard Statement

H302, H315, H319

Target

DYRK

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Metabolic Disease

Assay Protocol

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

Purity

99.67

Solubility

DMSO : 5 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

CCN1CCN(CC1)C(NC2=NC=CC(C3=CN(C4=CN=CC=C34)C5CCOCC5)=C2)=O

Molecular Formula

C24H30N6O2

Molecular Weight

434.53

Precautions

H302, H315, H319

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.

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

Available Sizes

Curated Selection

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