2. Metabolic Enzyme/Protease
  3. Fatty Acid Synthase (FASN)
  4. GSK2194069

GSK2194069 is a potent inhibitor of β-ketoyl reductase (KR) of fatty acid synthase (FASN), with an IC50 value of 7.7 nM. GSK2194069 shows specifically inhibitory effect on FAS expressing cancer cells, by acting potent efficacy on acetoacetyl-CoA, NADPH with IC50 or Ki values of 4.8 nM and 5.6 nM, respectively.

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GSK2194069 Chemical Structure

GSK2194069 Chemical Structure

CAS No. : 1332331-08-4

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 158 In-stock
Solution
10 mM * 1 mL in DMSO USD 158 In-stock
Solid
5 mg USD 144 In-stock
10 mg USD 252 In-stock
50 mg USD 708 In-stock
100 mg USD 1176 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 2 publication(s) in Google Scholar

GSK2194069 Related Antibodies

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  • Purity & Documentation

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Description

GSK2194069 is a potent inhibitor of β-ketoyl reductase (KR) of fatty acid synthase (FASN), with an IC50 value of 7.7 nM. GSK2194069 shows specifically inhibitory effect on FAS expressing cancer cells, by acting potent efficacy on acetoacetyl-CoA, NADPH with IC50 or Ki values of 4.8 nM and 5.6 nM, respectively[1][2][3].

In Vitro

GSK2194069 (100 nM; 24 h) inhibits fatty acid synthase (FAS) in cancer cell lines (KATO-III, MKN45, A549, SNU-1) without reducing FAS production protein level[1].
GSK2194069 decreases phosphatidylcholine levels in A549 cells with a half-maximum effective concentration (EC50) value of 15.5 ± 9 nM (n = 78), correlating with the decreased palmitate synthesis[1].
GSK2194069 (5 μM and 20 μM) shows higher efficacy in FASN-positive LNCaP cells rather than FASN-negative PC3 cells, with the higher FASN Expression level in LNCaP cells[2].
GSK2194069 (50 μM; 24 h) inhibits the growth of LNCaP-LN3 human prostate cancer cells[3].
GSK2194069 (60.4 nM; 24 h) displays properties of metabolomics, including L-acetyl carnitine, stearoyl carnitine, vaccenyl carnitine, and palmitoyl-L-carnitine decrease in LNCaP-LN3 cells[3].

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

GSK2194069 Related Antibodies

Western Blot Analysis[1]

Cell Line: A549
Concentration: 0, 10, 100, 1000 nM
Incubation Time: 48 hours or 120 hours
Result: Didn’t decrease FAS protein level.

Western Blot Analysis[2]

Cell Line: FASN-positive LNCaP cells, and FASN-negative PC3 cells
Concentration: 1 nM-0.1 mM
Incubation Time: 48 hours
Result: Inhibited tumor cells growth significantly, and reduced LNCaP cells much better.
Molecular Weight

428.48

Formula

C25H24N4O3
CAS No.
Appearance

Solid

Color

Light yellow to khaki

SMILES

O=C(N1C[C@H](CC2=NNC(N2C3=CC=C(C4=CC=C(OC=C5)C5=C4)C=C3)=O)CC1)C6CC6
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 : ≥ 100 mg/mL (233.38 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 2.3338 mL 11.6692 mL 23.3383 mL
5 mM 0.4668 mL 2.3338 mL 4.6677 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)

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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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: ≥ 2.5 mg/mL (5.83 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.83 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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:

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mg/kg

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(per animal)

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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 2.3338 mL 11.6692 mL 23.3383 mL 58.3458 mL
5 mM 0.4668 mL 2.3338 mL 4.6677 mL 11.6692 mL
10 mM 0.2334 mL 1.1669 mL 2.3338 mL 5.8346 mL
15 mM 0.1556 mL 0.7779 mL 1.5559 mL 3.8897 mL
20 mM 0.1167 mL 0.5835 mL 1.1669 mL 2.9173 mL
25 mM 0.0934 mL 0.4668 mL 0.9335 mL 2.3338 mL
30 mM 0.0778 mL 0.3890 mL 0.7779 mL 1.9449 mL
40 mM 0.0583 mL 0.2917 mL 0.5835 mL 1.4586 mL
50 mM 0.0467 mL 0.2334 mL 0.4668 mL 1.1669 mL
60 mM 0.0389 mL 0.1945 mL 0.3890 mL 0.9724 mL
80 mM 0.0292 mL 0.1459 mL 0.2917 mL 0.7293 mL
100 mM 0.0233 mL 0.1167 mL 0.2334 mL 0.5835 mL
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GSK2194069 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:

GSK21940691332331-08-4GSK 2194069GSK-2194069Fatty Acid Synthase (FASN)acetoacetyl-CoANADPHKATO-IIIMKN45A549SNU-1phosphatidylcholineFASN-positive LNCaP cellsFASN-negative PC3 cellsL-acetyl carnitinestearoyl carnitinevaccenyl carnitinepalmitoyl-L-carnitineInhibitorinhibitorinhibit

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