GNF2133 hydrochloride

Name: GNF2133 hydrochloride
Brand: MedChemExpress
SKU: HY-142295A
Rating: 4.5 (1 reviews)

Cat. No.: HY-142295A Purity: 99.29%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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.

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

CAS No. : 2561414-57-9

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in Water	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of GNF2133 hydrochloride:

GNF2133 In-stock

1 Publications Citing Use of MCE GNF2133 hydrochloride

•Nat Genet. 2025 Jun;57(6):1478-1492. [Abstract]

Cell Proliferation/Viability Assay

Flow Cytometry

: GNF2133 hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Genet. 2025 Jun;57(6):1478-1492. [Abstract]; Dose-dependent reduction of HEL cell proliferation in culture with the DYRK1A inhibitor GNF2133 (0.01, 0.1, 5, 10 μM).

: GNF2133 hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Genet. 2025 Jun;57(6):1478-1492. [Abstract]; Representative flow cytometry plots for Annexin V PI apoptosis assay demonstrating synergy between the DYRK1A inhibitor GNF2133 (‘GNF”) (100 nM) and the BCL2/BCL-XL inhibitor navitoclax (“NAV”).

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•Related Screening Libraries:

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View All DYRK Isoform Specific Products:

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DYRK1 DYRK2 DYRK3 DYRK4 HIPK PRP4

Biological Activity
Purity & Documentation
References
Customer Review

Description

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	/	/
V_{ss (L/kg)}	11	/	/
AUC (h·nM)	3268	10974	144420
C_max(nM)	1977	1675	13319
t_max<(h)	0.03	3.0	3.0
C_last(nM)	36.6	19	1324
t_1/2<(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.

2561414-57-9

Appearance

Solid

Color

Off-white to light brown

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

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

Solvent & Solubility

In Vitro:

H₂O : 100 mg/mL (212.32 mM; Need ultrasonic)

DMSO : 4 mg/mL (8.49 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	2.1232 mL	10.6159 mL	21.2319 mL
5 mM	0.4246 mL	2.1232 mL	4.2464 mL
10 mM	0.2123 mL	1.0616 mL	2.1232 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.4 mg/mL (0.85 mM); Clear solution

This protocol yields a clear solution of ≥ 0.4 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (4.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.4 mg/mL (0.85 mM); Clear solution

This protocol yields a clear solution of ≥ 0.4 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (4.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 0.4 mg/mL (0.85 mM); Clear solution

This protocol yields a clear solution of ≥ 0.4 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (4.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.86%

Select Batch:

Data Sheet (282 KB) SDS (251 KB)

COA (254 KB) HNMR (145 KB) RP-HPLC (169 KB) LCMS (234 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / H₂O	1 mM	2.1232 mL	10.6159 mL	21.2319 mL	53.0797 mL
DMSO / H₂O	5 mM	0.4246 mL	2.1232 mL	4.2464 mL	10.6159 mL
H₂O	10 mM	0.2123 mL	1.0616 mL	2.1232 mL	5.3080 mL
	15 mM	0.1415 mL	0.7077 mL	1.4155 mL	3.5386 mL
	20 mM	0.1062 mL	0.5308 mL	1.0616 mL	2.6540 mL
	25 mM	0.0849 mL	0.4246 mL	0.8493 mL	2.1232 mL
	30 mM	0.0708 mL	0.3539 mL	0.7077 mL	1.7693 mL
	40 mM	0.0531 mL	0.2654 mL	0.5308 mL	1.3270 mL
	50 mM	0.0425 mL	0.2123 mL	0.4246 mL	1.0616 mL
	60 mM	0.0354 mL	0.1769 mL	0.3539 mL	0.8847 mL
	80 mM	0.0265 mL	0.1327 mL	0.2654 mL	0.6635 mL
	100 mM	0.0212 mL	0.1062 mL	0.2123 mL	0.5308 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.