2. Protein Tyrosine Kinase/RTK
  3. DYRK
  4. 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.

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GNF2133 hydrochloride Chemical Structure

GNF2133 hydrochloride Chemical Structure

CAS No. : 2561414-57-9

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Description

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].

IC50 & Target[1]

DYRK1A

0.0062 μM (IC50)

GSK3β

>50 μM (IC50)

In Vivo

GNF2133 hydrochloride (30 mg/kg; p.o.) shows good oral absorption with oral bioavailability of 22.3%[1].
GNF2133 hydrochloride (30 mg/kg; p.o.; once a day for 5 days) shows the ability to proliferate β-cells in vivo[1].
GNF2133 hydrochloride (3, 10, 30 mg/kg) significantly improves glucose disposal capacity and increased insulin secretion in RIP-DTA mice[1].
Pharmacokinetic Parameters of GNF2133 hydrochloride in CD-1 mice[1].

plasma (iv) plasma (po) pancreas (po)
CL (mL/min/kg) 23.5 / /
Vss (L/kg) 11 / /
AUC (h·nM) 3268 10974 144420
Cmax(nM) 1977 1675 13319
tmax<(h) 0.03 3.0 3.0
Clast(nM) 36.6 19 1324
t1/2<(h) 6.6 3.4 6.6
F (%) / 22.3 /
CD-1 mice; 30 mg/kg; p.o.[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CD-1 mice[1]
Dosage: 30 mg/kg
Administration: P.o.
Result: Showed good oral absorption and moderate plasma exposure with oral bioavailability of 22.3%.
Animal Model: Wistar Han rat[1]
Dosage: 30 mg/kg (0.5% methylcellulose + Tween-80)
Administration: P.o.; once a day for 5 days
Result: Increased cyclin D1 levels and overall cell density, and increased in cell proliferation marker Ki67 and insulin.
Animal Model: Diphtheria toxin A (RIP-DTA) mice[1]
Dosage: 3, 10, 30 mg/kg (20 mg/kg doxycycline (Dox) for 5 days)
Administration: P.o., once a day for 35 days
Result: Significantly improves glucose disposal capacity and increased insulin secretion.
Molecular Weight

470.99

Formula

C24H31ClN6O2
CAS No.
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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GNF2133 hydrochloride Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GNF21332561414-57-9GNF 2133GNF-2133DYRKDual specificity tyrosine phosphorylation regulated kinaseDual specificity tyrosine regulated kinaseorally activeβ-cellglucose disposalinsulin secretionCD-1 miceRIP-DTA miceInhibitorinhibitorinhibit

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