Cat. No.: HY-129492

GNF4877

1 Cited Publications

Customer Review

Based on 1 publication(s) in Google Scholar

GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC₅₀s of 6 nM and 16 nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC₅₀ of 0.66 μM for mouse β (R7T1) cells).

For research use only. We do not sell to patients.

Purity: 99.82%
CAS No.: 2041073-22-5
Formula: C₂₅H₂₇FN₆O₄
Molecular Weight:494.52

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

GNF4877 Chemical Structure

CAS No.: 2041073-22-5

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

GSK3β

16 nM (IC₅₀)

DYRK1A

6 nM (IC₅₀)

All DYRK Isoforms :

All GSK-3 Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HT-22	IC₅₀	16.3 μM Compound: 12; GNF-4877	Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	[PMID: 36876904]
Pancreatic beta cell	EC₅₀	0.19 μM Compound: GNF4877	Induction of cell proliferation in rat beta cells incubated for 4 days by EdU incorporation assay Induction of cell proliferation in rat beta cells incubated for 4 days by EdU incorporation assay	[PMID: 32077280]
Pancreatic beta cell	EC₅₀	0.54 μM Compound: GNF4877	Induction of cell proliferation in human beta cells incubated for 4 days by EdU incorporation assay Induction of cell proliferation in human beta cells incubated for 4 days by EdU incorporation assay	[PMID: 32077280]

In Vitro

High glucose concentrations and glucokinase activators (GKAs) increase Ca²⁺ signalling in β-cells, and increase intracellular Ca²⁺ leads to activation of calcineurin and nuclear translocation of NFATc proteins. Indeed, concentrations of GNF4877 ((0.1 μM, 0.3 μM) well below the EC₅₀ for β-cell proliferation are able to induce proliferation in the presence of high glucose or pharmacological activators of glucokinase. Finally, increasing intracellular Ca²⁺ with glibenclamide (a sulfonylurea receptor 1 inhibitor) or Bay K8644 (an L-type Ca²⁺ channel activator) show additive activity with GNF4877^[1].

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

In Vivo

GNF4877 (50 mg/kg; oral gavage; twice a day; for 15 days; double transgenic RIP-DTA male mice) treatment induces β-cell proliferation, increases β-cell mass and insulin content, and improves glycaemic control^[1].

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

Animal Model:

Double transgenic RIP-DTA male mice (Tg (Ins 2-rtTA) 2 Efr Tg (teto-DTA) 1 Gfi/J) with Doxycycline (28.8±2.4 g; 82±2 days)^[1]
Dosage:

50 mg/kg
Administration:

Oral gavage; twice a day; for 15 days
Result:

Induced β-cell proliferation, increased β-cell mass and insulin content, and improved glycaemic control.

Chemical Information

CAS No. 2041073-22-5
Appearance Solid
Molecular Weight 494.52
Formula C₂₅H₂₇FN₆O₄
Color Light yellow to yellow
SMILES

O=C([C@H]1CN(C2=C(NC(C3=NC(C4=CC(OC(C)C)=CC=C4F)=CN=C3N)=O)C=NC=C2)CCC1)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

Publications (1)

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Journal Impact Factor

Nat Commun

CRISPR-based genome editing in primary human pancreatic islet cells. [Abstract]

2021 Apr 23;12(1):2397. PMID: 33893274

Solvent & Solubility

In Vitro:

DMSO : 3.33 mg/mL (6.73 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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0222 mL

10.1108 mL

20.2216 mL

5 mM

0.4044 mL

2.0222 mL

4.0443 mL

10 mM

---

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

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

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Shen W, et al. Inhibition of DYRK1A and GSK3β induces human β-cell proliferation. Nat Commun. 2015 Oct 26;6:8372. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.0222 mL	10.1108 mL	20.2216 mL	50.5541 mL
DMSO	5 mM	0.4044 mL	2.0222 mL	4.0443 mL	10.1108 mL

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GNF4877

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Publications Citing Use of MedChemExpress (MCE) GNF4877

All DYRK Isoforms

All GSK-3 Isoforms