GNF2133

SKU: orb1303298

Description

GNF2133 is a potent and selective DYRK1A inhibitor with an IC50 of 6.2 nM. It is a valuable research tool for studying type 1 diabetes, applicable in both in vitro enzymatic assays and in vivo models to investigate beta-cell proliferation and survival pathways.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 2561414-56-8
• MW: 434.53
• Purity: 98.51% (May vary between batches)
• Formula: C₂₄H₃₀N₆O₂
• SMILES: CCN1CCN(CC1)C(=O)Nc1cc(ccn1)-c1cn(C2CCOCC2)c2cnccc12
• Target: DYRK
• Solubility: DMSO:4.5 mg/mL (10.36 mM)

Bioactivity

• Target IC50:
  GSK-3β:>50 μM|DYRK1A:0.0062 μM
• In Vivo:
  In Diphtheria toxin A (RIP-DTA) mice, GNF2133 (3, 10, 30 mg/kg) significantly improves glucose disposal capacity and increased insulin secretion. In CD-1 mice, GNF2133 (30 mg/kg; p.o.) shows moderate plasma exposure and good oral absorption with oral bioavailability of 22.3%. In Wistar Han rat, GNF2133 (30 mg/kg; p.o.) increases in cell proliferation marker Ki67 and insulin and reduces cyclin D1 levels and overall cell density.
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• In Vitro:
  GNF2133 has an IC50 of >50 µM for GSK3β. GNF2133 significantly improves glucose disposal capacity and increases insulin secretion.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Dual specificity tyrosine regulated kinase, Dual specificity tyrosine phosphorylation regulated kinase, DYRK1A, DYRK, CD-1 mice, orally active, Inhibitor, inhibit, insulin secretion, GNF2133, GNF-2133, GNF 2133, glucose disposal, RIP-DTA mice, β-cell

Compound Identifiers

PubChem CID

145994392