2. Stem Cell/Wnt
  3. Porcupine
  4. GNF-6231

GNF-6231 is a porcupine (IC50= 0.8 nM), Pron, and endoplasmic reticulum protein inhibitor with oral activity. GNF-6231 has anticancer activity. GNF-6231 can prevent the activation of the Wnt pathway by blocking the secretion of all Wnt ligands. GNF-6231 can be used in the study of myocardial infarction.

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GNF-6231 Chemical Structure

GNF-6231 Chemical Structure

CAS No. : 1243245-18-2

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10 mM * 1 mL in DMSO
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10 mg USD 130 In-stock
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Based on 1 publication(s) in Google Scholar

GNF-6231 Related Antibodies

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  • Purity & Documentation

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Description

GNF-6231 is a porcupine (IC50= 0.8 nM), Pron, and endoplasmic reticulum protein inhibitor with oral activity. GNF-6231 has anticancer activity. GNF-6231 can prevent the activation of the Wnt pathway by blocking the secretion of all Wnt ligands. GNF-6231 can be used in the study of myocardial infarction[1][2][3][4].

In Vitro

GNF-6231 inhibits Porcupine enzyme activity with IC50 0.8 nM and isn’t cytotoxic in the concentration range of 20 μM[1].

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

GNF-6231 Related Antibodies
In Vivo

GNF-6231 (5 mg/kg; Intravenous injection (i.v.); every 24 hours for 6 days) alleviates the symptoms of myocardial infarction in C57Bl/6 mice by inhibiting the activation of the Wnt pathway[1].
GNF-6231 (0.3-3 mg/kg; p.o.; once daily for 2 weeks) shows antitumor activity in a mouse of MMTV-WNT1 xenograft tumor[4].

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

Animal Model: C57Bl/6 mice model of myocardial infarction[1]
Dosage: 5 mg/kg
Administration: Intravenous injection (i.v.); Starting from 6 hours after myocardial infarction surgery to the sixth day after infarction, once every 24 hours
Result: Reduced nuclear and cytoplasmic β-catenin levels.
Reduced adverse cardiac remodeling and reduced myocardial infarction area in mice (9.07%).
Enhanced the overall heart repair and recovery after left ventricular infarction.
Animal Model: Mouse MMTV-WNT1 xenograft tumor model[2]
Dosage: 0.3 mg/kg,1.0 mg/kg, 3 mg/kg
Administration: Oral gavage; Once daily for 2 weeks
Result: At a single dose of 3 mg/kg, reduced the level of Wnt target gene Axin2 mRNA.
Promoted tumor regression in mice in a dose-dependent manner.
Molecular Weight

448.49

Formula

C24H25FN6O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=NC=C(N2CCN(C(C)=O)CC2)C=C1)CC3=CN=C(C4=CC(F)=NC=C4)C(C)=C3
Shipping

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

DMSO : ≥ 36 mg/mL (80.27 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2297 mL 11.1485 mL 22.2970 mL
5 mM 0.4459 mL 2.2297 mL 4.4594 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 3 mg/mL (6.69 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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: ≥ 3 mg/mL (6.69 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2297 mL 11.1485 mL 22.2970 mL 55.7426 mL
5 mM 0.4459 mL 2.2297 mL 4.4594 mL 11.1485 mL
10 mM 0.2230 mL 1.1149 mL 2.2297 mL 5.5743 mL
15 mM 0.1486 mL 0.7432 mL 1.4865 mL 3.7162 mL
20 mM 0.1115 mL 0.5574 mL 1.1149 mL 2.7871 mL
25 mM 0.0892 mL 0.4459 mL 0.8919 mL 2.2297 mL
30 mM 0.0743 mL 0.3716 mL 0.7432 mL 1.8581 mL
40 mM 0.0557 mL 0.2787 mL 0.5574 mL 1.3936 mL
50 mM 0.0446 mL 0.2230 mL 0.4459 mL 1.1149 mL
60 mM 0.0372 mL 0.1858 mL 0.3716 mL 0.9290 mL
80 mM 0.0279 mL 0.1394 mL 0.2787 mL 0.6968 mL
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GNF-6231 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:

GNF-62311243245-18-2GNF6231GNF 6231PorcupineHeart failureMyocardial infarctionWntapoptosisproliferationWNT/β-Catenin PathwayMMTV-Wnt1 tumerInhibitorinhibitorinhibit

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