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

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GNF2133 Chemical Structure

GNF2133 Chemical Structure

CAS No. : 2561414-56-8

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Based on 1 publication(s) in Google Scholar

Other Forms of GNF2133:

GNF2133 Related Antibodies

Top Publications Citing Use of Products

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DYRK1 DYRK2 DYRK3 DYRK4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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].

IC50 & Target[1]

DYRK1A

0.0062 μM (IC50)

GSK3β

>50 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
CHO IC50
> 30 μM
Compound: 13g; GNF2133
Displacement of [3H]dofetilide from human ERG expressed in CHO cells incubated for 90 mins by microbeta scintillation counting method
Displacement of [3H]dofetilide from human ERG expressed in CHO cells incubated for 90 mins by microbeta scintillation counting method
[PMID: 32077280]
Pancreatic beta cell EC50
0.21 μM
Compound: 13g; GNF2133
Induction of cell proliferation in human beta cells incubated for 96 hrs by EdU incorporation assay
Induction of cell proliferation in human beta cells incubated for 96 hrs by EdU incorporation assay
[PMID: 32077280]
Pancreatic beta cell EC50
0.4 μM
Compound: 13g; GNF2133
Induction of cell proliferation in rat beta cells incubated for 96 hrs by EdU incorporation assay
Induction of cell proliferation in rat beta cells incubated for 96 hrs by EdU incorporation assay
[PMID: 32077280]
Sf21 IC50
0.0062 μM
Compound: 13g; GNF2133
Inhibition of recombinant human N-terminal GST-tagged DYRK1A (1 to 763 residues) expressed in Sf21 cells using Ulight-glycogen synthase as substrate incubated for 60 mins by TR-FRET LANCE method
Inhibition of recombinant human N-terminal GST-tagged DYRK1A (1 to 763 residues) expressed in Sf21 cells using Ulight-glycogen synthase as substrate incubated for 60 mins by TR-FRET LANCE method
[PMID: 32077280]
Sf9 IC50
> 50 μM
Compound: 13g; GNF2133
Inhibition of recombinant human His/GST-tagged GSK3beta (2 to 433 residues) expressed in baculovirus infected Sf9 cells using Ulight-glycogen synthase peptide as substrate incubated for 30 mins by TR-FRET LANCE method
Inhibition of recombinant human His/GST-tagged GSK3beta (2 to 433 residues) expressed in baculovirus infected Sf9 cells using Ulight-glycogen synthase peptide as substrate incubated for 30 mins by TR-FRET LANCE method
[PMID: 32077280]
In Vivo

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

434.53

Formula

C24H30N6O2
CAS No.
Appearance

Solid

Color

Off-white to pink

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 4 mg/mL (9.21 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3013 mL 11.5067 mL 23.0134 mL
5 mM 0.4603 mL 2.3013 mL 4.6027 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.49%

SDS (251 KB)

COA (253 KB) HNMR (144 KB) RP-HPLC (163 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3013 mL 11.5067 mL 23.0134 mL 57.5334 mL
5 mM 0.4603 mL 2.3013 mL 4.6027 mL 11.5067 mL
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GNF2133 Related Classifications

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:

GNF21332561414-56-8GNF 2133GNF-2133DYRKDual specificity tyrosine phosphorylation regulated kinaseDual specificity tyrosine regulated kinaseorally activeβ-cellglucose disposalinsulin secretionCD-1 miceRIP-DTA miceInhibitorinhibitorinhibit

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