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GSK2194069 | Inhibitor of FASN
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

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Targets Biochemical/Biophysical Potency Cellular Potency
FASN
  • IC50: 7.7 ± 4.1 nM
  • Ki:5 nM
  • EC50:15.5 ± 9 nM
Inhibitor
100 nM

Selectivity

Potency
Cellular
In Vitro

FASN

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1038/nchembio.1603

In Vivo Validations

Mouse
Dose: 3 mg/Kg
Route of delivery: Oral

DOI Reference: 10.1038/nchembio.1603

Chemical Information

Molecular Formula C25H24N4O3
SMILEs O=C(C1CC1)N1CC[C@@H](Cc2n[nH]c(=O)n2-c2ccc(-c3ccc4occc4c3)cc2)C1
InChI InChI=1S/C25H24N4O3/c30-24(18-1-2-18)28-11-9-16(15-28)13-23-26-27-25(31)29(23)21-6-3-17(4-7-21)19-5-8-22-20(14-19)10-12-32-22/h3-8,10,12,14,16,18H,1-2,9,11,13,15H2,(H,27,31)/t16-/m0/s1
Molecular weight 428.18 Da
AlogP 0.0
HBond acceptors 7
HBond donors 1
Atoms 56

Vendors

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Expert Reviews

by SERP
(on 7 Sept 2021)
Cellular Use Rating
In Model Organisms
An excellent probe for FASN but, as PK data is missing, it is hard to judge the in vivo dosing.
by SERP
(on 13 Sept 2021)
Cellular Use Rating
In Model Organisms
GSK2194069 is a potent probe for the beta-ketoacyl reductase domain of hFAS, and has the potential to be useful in exploring the role of fatty acid synthesis in tumour proliferation. Its inhibition...
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