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

GSK2194069 

Cat. No.: HY-12325 Purity: 99.84%
COA Handling Instructions

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.

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

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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Customer Review

Based on 2 publication(s) in Google Scholar

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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.

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)

*"≥" 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
10 mM 0.2334 mL 1.1669 mL 2.3338 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation
References
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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.

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Product Name:
GSK2194069
Cat. No.:
HY-12325
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