Home Metabolism FXR agonist - Autophagy activator GW4064 For research use only.

GW4064

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.

GW4064 Chemical Structure

GW4064 Chemical Structure

CAS: 278779-30-9

Selleck's GW4064 has been cited by 29 Publications

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Purity & Quality Control

Batch: Purity: 99.80%
99.80

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 Function assay Agonistic activity at FXR in HEK293 cells by GAL4 transactivation activity, EC50 = 0.07 μM. 17292610
CV1 Function assay Agonist activity at FXR expressed in african green monkey CV1 cells by luciferase reporter transient transfection assay, EC50 = 0.065 μM. 18621523
CV1 Function assay Agonist activity at human FXR transfected in african green monkey CV1 cells by luciferase reporter gene transient transfection assay, EC50 = 0.065 μM. 19410460
CV1 Function assay Increase in human FXR-mediated transient transcription of luciferase reporter gene transfected in african green monkey CV1 cells, EC50 = 0.065 μM. 19586769
HEK293 Function assay Agonist activity at human full length FXR transfected in HEK293 cells coexpressing pTRexDest/pGL2promotor assessed as luciferase activity by direct reporter cellular assay, EC50 = 0.03 μM. 20638278
HEK293 Function assay Agonist activity at human GST-fused FXR LBD expressed in HEK293 cells coexpressing GAL4-DNA bindig domain and pFRluc by mammalian one-hybrid assay, EC50 = 0.035 μM. 20638278
CV-1 Function assay Agonist activity at human FXR LBD iexpressed in monkey CV-1 cells assessed as transactivation of luciferase reporter gene expression, EC50 = 0.065 μM. 21256005
CV1 Function assay Agonist activity at human FXR LBD transfected in african green monkey CV1 cells after overnight incubation by luciferase reporter gene assay, EC50 = 0.065 μM. 21890356
HEK293 Function assay Agonist activity at human recombinant FXR expressed in HEK293 cells coexpressing CMX-GAL4N by luciferase reporter gene assay, EC50 = 0.07 μM. 22583617
HEK293 Function assay Agonist activity at human FXR expressed in HEK293 cells by luciferase reporter gene assay, EC50 = 0.026 μM. 25305688
CV1 Function assay Agonist activity at FXR (unknown origin) transfected into african green monkey CV1 cells assessed as ligand-mediated transcription by luciferase reporter/ transient transfection assay, EC50 = 0.065 μM. 25499883
HeLa Function assay 24 hrs Agonist activity at human full length FXR expressed in HeLa cells cotransfected with pSG5-human RXR after 24 hrs by Dual-Glo luciferase reporter gene assay, EC50 = 0.51 μM. 25934227
HEK293 Function assay Agonist activity at human FXR transfected in HEK293 cells assessed as transcriptional activity by luciferase reporter gene assay, EC50 = 0.373 μM. 26568144
HEK-293 Function assay Agonist activity at C-terminal Gal4-tagged human FXR (187 to 472 residues) expressed in HEK-293 cells co-expressing pFRluc by mammalian one hybrid assay, EC50 = 0.035 μM. 27268696
insect cells Function assay 1 hr Agonist activity at recombinant human GST-tagged FXR ligand binding domain (193 to 472 residues) expressed in baculovirus infected insect cells assessed as induction of interaction with biotin labelled SRC-1 after 1 hr by HTRF assay, EC50 = 0.019 μM. 29148806
HEK293T Function assay 24 hrs Agonist activity at human FXR expressed in HEK293T cells assessed as BSEP promoter driven cellular transcriptional activity after 24 hrs by luciferase reporter gene assay, EC50 = 0.095 μM. 29148806
HepG2 Function assay 1 uM 18 hrs Decrease in CYP7A1 gene expression in human HepG2 cells at 1 uM after 18 hrs by RT-PCR 17963371
Caco-2 Function assay 1 uM 6 days Activation of IBABP gene expression in human Caco-2 cells at 1 uM after 6 days by RT-PCR 17963371
HepG2 Function assay 1 uM 18 hrs Activation of BSEP gene expression in human HepG2 cells at 1 uM after 18 hrs by RT-PCR 17963371
Huh7 Function assay 1 uM 18 hrs Activation of SHP gene expression in human Huh7 cells at 1 uM after 18 hrs by RT-PCR 17963371
Huh7 Function assay 1 uM 18 hrs Activation of BSEP gene expression in human Huh7 cells at 1 uM after 18 hrs by RT-PCR 17963371
HepG2 Function assay 10 uM Induction of FXR-mediated SHP mRNA expression in serum-starved human HepG2 cells at 10 uM measured after overnight incubation by qPCR analysis 27372840
HepG2 Function assay 10 uM 10 mins Induction of FXR-mediated Akt-phosphorylation at S473 site in serum-starved human HepG2 cells at 10 uM measured after 10 mins by western blot analysis 27372840
HepG2 Function assay 10 uM 10 mins Induction of FXR-mediated Akt-phosphorylation in serum-starved human HepG2 cells assessed as increase in GSK-3beta-phosphorylation at 10 uM measured after 10 mins by western blot analysis 27372840
HepG2 Function assay 10 uM Activation of FXR in human HepG2 cells assessed as upregulation of SHP mRNA expression at 10 uM by RT-PCR method 30031618
HepG2 Function assay 10 uM Activation of FXR in human HepG2 cells assessed as upregulation of FXR mRNA expression at 10 uM by RT-PCR method 30031618
HepG2 Function assay 10 uM Activation of FXR in human HepG2 cells assessed as downregulation of SREBP-1c mRNA expression at 10 uM by RT-PCR method 30031618
3T3L1 Function assay 10 uM Reduction in lipid accumulation in mouse 3T3L1 cells at 10 uM by Oil Red O staining-based absorbance method relative to control 30342957
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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
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]
Kinase Assay FXR Transient Transfection Assay
CV1 cells are maintained in DMEM high glucose medium. The CV1 cells are harvested 72 hours before transfection and plated in DMEM-F12 phenol red free medium containing 5% charcoal/dextran treated fetal bovine serum and 2 mM glutamine. On the day of transfection, the CV1 cells are harvested in DMEM-F12 phenol red free medium containing 5% charcoal/dextran treated fetal bovine serum and 2 mM glutamine, counted and seeded into a T-175 cm2 flask at a density of 14 million cells per flask before adding the transfection mix. The FuGENE® 6 transfection mix containing 0.55 μg pFA-CMV-GAL4-human FXR LBD expression plasmid, 10.92 μg of the (UAS)-tk-Luciferase reporter plasmid, 20.75 μg of pBluescript II KS+, and 3.82 μg of a human steroid receptor co-activator (SRC-1) construct is incubated and then added to the CV1 cells for overnight incubation in incubator. The transfected CV1 cells are harvested in DMEM-F12 phenol red free medium containing 5% charcoal/dextran treated fetal bovine serum and 2 mM glutamine. Transfected cells are added at a concentration of 3750 cells/well to 384-well plates containing ligands. Luciferase expression is measured using Steady-Glo?Luciferase Assay System 24 hr after incubation with ligand. GW4064X is used as the control, and data are normalized to GW4064X as % control.
Cell Research Cell lines HepG2 cells
Concentrations 10 µM
Incubation Time 2 h
Method

Cells were treated with indicated concentration of drug for 2 h.
Experimental Result Images Methods Biomarkers Images PMID
Western blot PTEN / p-AKT / AKT p-EGFR / EGFR / p-ERK / ERK / p-Src / Src SOCS3 / p21 / p-STAT3 / STAT3 25187826
Growth inhibition assay Cell proliferation 25187826
In Vivo
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 Animal Models Fisher rats
Dosages 0-100 mg/kg
Administration Orally, b.i.d.

Chemical Information & Solubility

Molecular Weight 542.84 Formula

C28H22Cl3NO4
CAS No. 278779-30-9 SDF Download GW4064 SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (184.21 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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