GW4064

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.

Size Price Stock Quantity  
10mM (1mL in DMSO) EUR 147 In stock
EUR 68 In stock
EUR 108 In stock
EUR 265 In stock
EUR 363 In stock
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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.
Targets
FXR [1]
(CV1)
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 MYLGeY5kfGmxbjDhd5NigQ>? MnewRYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDGXHIh\XiycnXzd4VlKGmwIFjFT|I6OyClZXzsd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGVEPTB;MD6wNlYh|ryP MUeyOVMxPTZ6OB?=
monkey CV-1 cells M3vU[2Z2dmO2aX;uJIF{e2G7 NGG0VHhC\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJGZZWiCOQlSgbYV5eHKnc4Pl[EBqdiCvb37r[ZkhS1ZvMTDj[YxteyCjc4Pld5Nm\CCjczD0doFve2GldHn2ZZRqd25ib3[gcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHX4dJJme3Orb36sJGVEPTB;MD6wOlUh|ryP NHewVWszOTJ3NkCwOS=>
HEK293 cells MVfGeY5kfGmxbjDhd5NigQ>? MXfB[49vcXO2aXOgZYN1cX[rdImgZZQhTliUIHnuJGhGUzJ7MzDj[YxteyCkeTDHRWw1KHS{YX7zZYN1cX[jdHnvckBi[3Srdnn0fUwhTUN3ME2wMlA4KM7:TR?= MoniNVczQTJ4MUC=
HeLa cells NXKyOW9UTnWwY4Tpc44h[XO|YYm= NFzENHgzPCCq MYHB[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIH\1cIwhdGWwZ4ToJGZZWiCneIDy[ZN{\WRiaX6gTIVN[SClZXzsd{Bkd3S{YX7z[oVkfGWmIIfpeIgheFOJNT3oeY1idiCUWGKgZYZ1\XJiMkSgbJJ{KGK7IFT1ZYwuT2yxIHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhTUN3ME2wMlUyKM7:TR?= MXWyOVk{PDJ{Nx?=
human Caco-2 cells M{D6RWZ2dmO2aX;uJIF{e2G7 NWfYc3JuOSEQvF2= M4DtSVYh\GG7cx?= MlG0RYN1cX[jdHnvckBw\iCLQlHCVEBo\W6nIHX4dJJme3Orb36gbY4hcHWvYX6gR4Fkdy1{IHPlcIx{KGG2IEGgeW0h[W[2ZYKgOkBl[Xm|IHL5JHJVNVCFUh?= MYOxO|k3OzN5MR?=
human HepG2 cells MkKwSpVv[3Srb36gZZN{[Xl? MY[xJO69VQ>? M1WxVFE5KGh? NHHPNWRF\WO{ZXHz[UBqdiCFWWC3RVEh\2WwZTDlfJBz\XO|aX;uJIlvKGi3bXHuJGhmeEd{IHPlcIx{KGG2IEGgeW0h[W[2ZYKgNVghcHK|IHL5JHJVNVCFUh?= MmPsNVc6PjN|N{G=
human HepG2 cells NXPLcIxGTnWwY4Tpc44h[XO|YYm= M1rsOlEh|ryP Ml75NVghcA>? NI\6WpNF\WO{ZXHz[UBqdiCFWWC3RVEh\2WwZTDlfJBz\XO|aX;uJIlvKGi3bXHuJGhmeEd{IHPlcIx{KGG2IEGgeW0h[W[2ZYKgNVghcHK|IHL5JHJVNVCFUh?= MUSxO|k3OzN5MR?=
human Huh7 cells MlfwSpVv[3Srb36gZZN{[Xl? NYLuW5lDOSEQvF2= NFHLVZEyQCCq M1jzeWFkfGm4YYTpc44hd2ZiU1jQJIdmdmViZYjwdoV{e2mxbjDpckBpfW2jbjDIeYg4KGOnbHzzJIF1KDFidV2gZYZ1\XJiMUigbJJ{KGK7IGLUMXBEWg>? MmXDNVc6PjN|N{G=
human HepG2 cells M2jwVWZ2dmO2aX;uJIF{e2G7 M4fyXFEh|ryP M1PyeVE5KGh? MYHBZ5RqfmG2aX;uJI9nKEKVRWCg[4Vv\SCneIDy[ZN{cW:wIHnuJIh2dWGwIFjldGczKGOnbHzzJIF1KDFidV2gZYZ1\XJiMUigbJJ{KGK7IGLUMXBEWg>? M2nadVE4QTZ|M{ex
human Huh7 cells NFXC[|ZHfW6ldHnvckBie3OjeR?= MmDPNUDPxE1? Moj3NVghcA>? NXPoNnVJSWO2aY\heIlwdiCxZjDCV2VRKGenbnWg[ZhxemW|c3nvckBqdiCqdX3hckBJfWh5IHPlcIx{KGG2IEGgeW0h[W[2ZYKgNVghcHK|IHL5JHJVNVCFUh?= NYXnelJGOTd7NkOzO|E>

... Click to View More Cell Line Experimental Data

Assay
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. 

25187826
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]

Protocol

Animal Research:

[2]

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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
Formula

C28H22Cl3NO4

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