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GSK2194069

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Catalog No. T15429Cas No. 1332331-08-4

GSK2194069 is an active β-keto reductase (KR)-specific inhibitor of fatty acid synthase (FASN) with an IC50 of 7.7 nM in an assay for the detection of released CoA.GSK2194069 inhibits the proliferation of FAS in cancer cells through the action of acetoacetyl-coenzyme A and NADPH.

GSK2194069

GSK2194069

😃Good
Purity: 99.84%
Catalog No. T15429Cas No. 1332331-08-4
GSK2194069 is an active β-keto reductase (KR)-specific inhibitor of fatty acid synthase (FASN) with an IC50 of 7.7 nM in an assay for the detection of released CoA.GSK2194069 inhibits the proliferation of FAS in cancer cells through the action of acetoacetyl-coenzyme A and NADPH.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$71-In Stock
5 mg$118-In Stock
10 mg$198-In Stock
25 mg$377-In Stock
50 mg$586-In Stock
100 mg$973-In Stock
200 mg$1,290-In Stock
1 mL x 10 mM (in DMSO)$129-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.84%
Appearance:Solid
Color:White to Yellow
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Product Introduction

Bioactivity
Description
GSK2194069 is an active β-keto reductase (KR)-specific inhibitor of fatty acid synthase (FASN) with an IC50 of 7.7 nM in an assay for the detection of released CoA.GSK2194069 inhibits the proliferation of FAS in cancer cells through the action of acetoacetyl-coenzyme A and NADPH.
Targets&IC50
β-ketoyl reductase:7.7 nM, Phosphatidylcholine:15.5 ± 9 nM(EC50)
In vitro
GSK2194069 (100 nM; 24 h) suppresses fatty acid synthase (FAS) activity in cancer cell lines (KATO-III, MKN45, A549, SNU-1) while maintaining FAS protein production levels.[1] GSK2194069 (5 μM and 20 μM) demonstrates higher efficacy in FASN-positive LNCaP cells compared to FASN-negative PC3 cells, correlating with higher FASN expression 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) exhibits metabolomic alterations, including decreases in L-acetyl carnitine, stearoyl carnitine, vaccenyl carnitine, and palmitoyl-L-carnitine in LNCaP-LN3 cells.[3]
Chemical Properties
Molecular Weight428.48
FormulaC25H24N4O3
Cas No.1332331-08-4
SmilesO=C(C1CC1)N1CC[C@@H](Cc2n[nH]c(=O)n2-c2ccc(cc2)-c2ccc3occc3c2)C1
Relative Density.1.44 g/cm3 (Predicted)
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 90 mg/mL (210.04 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (7.7 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.3338 mL11.6692 mL23.3383 mL116.6916 mL
5 mM0.4668 mL2.3338 mL4.6677 mL23.3383 mL
10 mM0.2334 mL1.1669 mL2.3338 mL11.6692 mL
20 mM0.1167 mL0.5835 mL1.1669 mL5.8346 mL
50 mM0.0467 mL0.2334 mL0.4668 mL2.3338 mL
100 mM0.0233 mL0.1167 mL0.2334 mL1.1669 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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