For research use only.

Catalog No.S2782

19 publications

GW4064 Chemical Structure

CAS No. 278779-30-9

GW4064 is an agonist of farnesoid X receptor (FXR) with EC50 of 65 nM in CV1 cell line and displays no activity at other nuclear receptors at concentrations up to 1 μM. GW4064 stimulates autophagy in MCF-7 cells.

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Selleck's GW4064 has been cited by 19 publications

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Biological Activity

Description GW4064 is an agonist of farnesoid X receptor (FXR) with EC50 of 65 nM in CV1 cell line and displays no activity at other nuclear receptors at concentrations up to 1 μM. GW4064 stimulates autophagy in MCF-7 cells.
FXR [1]
65 nM(EC50)
In vitro

GW 4064 is a full agonist with EC50 values of 80 and 90 nM, respectively, in CV-1 cells transfected with mouse and human FXR expression vectors and an established reporter gene. There is no activity of GW 4064 on other nuclear receptors, including the retinoic acid receptor, at concentrations up to 1 μM. Thus, GW 4064 is a potent and selective nonsteroidal FXR agonist. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 cells Mnq2SpVv[3Srb36gZZN{[Xl? NW\SeFVuSWexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBHYFJiZYjwdoV{e2WmIHnuJGhGUzJ7MzDj[YxteyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEWFNUC9NE4xOjZizszN MmH4NlU{ODV4OEi=
monkey CV-1 cells M1;w[2Z2dmO2aX;uJIF{e2G7 MkfQRYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDGXHIhVEKGIHnlfJBz\XO|ZXSgbY4hdW:wa3X5JGNXNTFiY3XscJMh[XO|ZYPz[YQh[XNidILhcpNi[3SrdnH0bY9vKG:oIHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCneIDy[ZN{cW:wLDDFR|UxRTBwME[1JO69VQ>? NXviRVd7OjF{NU[wNFU>
HEK293 cells MXHGeY5kfGmxbjDhd5NigQ>? MkXVRYdwdmm|dHnjJIFkfGm4aYT5JIF1KE[[UjDpckBJTUt{OUOgZ4VtdHNiYomgS2FNPCC2cnHud4FkfGm4YYTpc44h[WO2aY\peJktKEWFNUC9NE4xPyEQvF2= NFHGblAyPzJ7Mk[xNC=>
HeLa cells NISzTnFHfW6ldHnvckBie3OjeR?= NGj6VFczPCCq MVzB[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIH\1cIwhdGWwZ4ToJGZZWiCneIDy[ZN{\WRiaX6gTIVN[SClZXzsd{Bkd3S{YX7z[oVkfGWmIIfpeIgheFOJNT3oeY1idiCUWGKgZYZ1\XJiMkSgbJJ{KGK7IFT1ZYwuT2yxIHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhTUN3ME2wMlUyKM7:TR?= MYSyOVk{PDJ{Nx?=
human Caco-2 cells MXTGeY5kfGmxbjDhd5NigQ>? M2m4elEh|ryP NI\vb4g3KGSjeYO= M3\vUGFkfGm4YYTpc44hd2ZiSVLBRnAh\2WwZTDlfJBz\XO|aX;uJIlvKGi3bXHuJGNi[29vMjDj[YxteyCjdDCxJJVOKGGodHXyJFYh\GG7czDifUBTXC2SQ2K= MWexO|k3OzN5MR?=
human HepG2 cells NXj5TmpnTnWwY4Tpc44h[XO|YYm= NGHofFEyKM7:TR?= NEnZfWsyQCCq MkDwSIVkemWjc3WgbY4hS1mSN1GxJIdmdmViZYjwdoV{e2mxbjDpckBpfW2jbjDI[ZBIOiClZXzsd{BifCBzIIXNJIFnfGW{IEG4JIhzeyCkeTDSWE1RS1J? MX2xO|k3OzN5MR?=
human HepG2 cells MnGySpVv[3Srb36gZZN{[Xl? Mn;6NUDPxE1? NUPiTIpOOThiaB?= MXzE[YNz\WG|ZTDpckBEYVB5QUGg[4Vv\SCneIDy[ZN{cW:wIHnuJIh2dWGwIFjldGczKGOnbHzzJIF1KDFidV2gZYZ1\XJiMUigbJJ{KGK7IGLUMXBEWg>? M1H3WFE4QTZ|M{ex
human Huh7 cells MWjGeY5kfGmxbjDhd5NigQ>? MnGxNUDPxE1? NVTMWGlOOThiaB?= NF;GPZZC[3SrdnH0bY9vKG:oIGPIVEBo\W6nIHX4dJJme3Orb36gbY4hcHWvYX6gTJVpPyClZXzsd{BifCBzIIXNJIFnfGW{IEG4JIhzeyCkeTDSWE1RS1J? M3e3OlE4QTZ|M{ex
human HepG2 cells M3rrbmZ2dmO2aX;uJIF{e2G7 Mo\iNUDPxE1? NXH1WGNDOThiaB?= MYTBZ5RqfmG2aX;uJI9nKEKVRWCg[4Vv\SCneIDy[ZN{cW:wIHnuJIh2dWGwIFjldGczKGOnbHzzJIF1KDFidV2gZYZ1\XJiMUigbJJ{KGK7IGLUMXBEWg>? NWDhXpNqOTd7NkOzO|E>
human Huh7 cells M{DWT2Z2dmO2aX;uJIF{e2G7 M{PQTVEh|ryP NWrR[2xUOThiaB?= M4DNfWFkfGm4YYTpc44hd2ZiQmPFVEBo\W6nIHX4dJJme3Orb36gbY4hcHWvYX6gTJVpPyClZXzsd{BifCBzIIXNJIFnfGW{IEG4JIhzeyCkeTDSWE1RS1J? NHL3UngyPzl4M{O3NS=>

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
PTEN / p-AKT / AKT ; 

PubMed: 25187826     

Protein expression levels of PTEN, phosphorylated and total Akt in LNcaP cells treated with a vehicle control (DMSO), CDCA or GW4064. 

p-EGFR / EGFR / p-ERK / ERK / p-Src / Src ; 

PubMed: 23119029     

A. Time-course and dose-response for GW4064-induced inhibition of EGFR (Tyr845) phosphorylation. B. Time-course and dose-response for GW4064-induced inhibition of ERK1/2 phosphorylation. C. Time-course and dose-response for GW4064-induced inhibition of Src (Tyr 416) phosphorylation. Phosphorylation of EGFR (Tyr845), ERK1/2 and Src (Tyr 416) was determined by immunoblotting with anti-phospho-EGFR (Tyr845), anti-phospho-ERK1/2 and anti-phospho-Src (Tyr 416) antibody, respectively. For time-course experiments, SNU-C4 cells were treated with 1 µM GW4064 for the indicated times at 37°C. For dose-response experiments, cells were treated with the indicated concentrations of GW4064 for 20 min at 37°C. Immunoblotting for total EGFR, ERK2 or Src was used as a loading control. Immunoblots are representative of at least 3 separate experiments. Numbers between immunoblots represent densitometry. Experimental/control ratios were calculated after normalizing each test band to the respective EGFR, ERK2 or Src band.

SOCS3 / p21 / p-STAT3 / STAT3 ; 

PubMed: 26416445     

HepG2 cells and Huh7 cells were treated with GW4064 (2 μM) or vehicle DMSO for 24 h. The protein levels of SOCS3, p21, total STAT3 (t-SATA3) and phosphoraylated STAT3 (p-STAT3) were assayed by Western blot, taking GAPDH as a loading control

25187826 23119029 26416445
Growth inhibition assay
Cell proliferation ; 

PubMed: 25187826     

LNcaP cells were treated with CDCA (5 μM), GW4064 (2 μM) or vehicle control (DMSO) and cell proliferation ability was measured using BrdU assays. A450 absorption was assayed following treatment for 24 h. 

In vivo Pharmacokinetic analysis in rats shows that GW 4064 possesses an oral bioavailability of 10% with a t1/2 = 3.5 h. Fisher rats are dosed with GW 4064 by oral gavage. After 7 days, a dose-dependent lowering of serum triglycerides is observed in the rats receiving GW 4064, with an ED50 = 20 mg/kg. [2]


Animal Research:


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  • Animal Models: Fisher rats
  • Dosages: 0-100 mg/kg
  • Administration: Orally, b.i.d.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (184.21 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% methylcellulose
For best results, use promptly after mixing.
11 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 542.84


CAS No. 278779-30-9
Storage powder
in solvent
Synonyms N/A
Smiles CC(C)C1=C(C(=NO1)C2=C(C=CC=C2Cl)Cl)COC3=CC(=C(C=C3)C=CC4=CC(=CC=C4)C(=O)O)Cl

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID