GW3965 HCl

For research use only.

Catalog No.S2630

23 publications

GW3965 HCl Chemical Structure

CAS No. 405911-17-3

GW3965 HCl is a potent, selective LXR agonist for hLXRα and hLXRβ with EC50 of 190 and 30 nM in cell-free assays, respectively.

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10mM (1mL in DMSO) EUR 235 In stock
EUR 95 In stock
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Selleck's GW3965 HCl has been cited by 23 publications

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Biological Activity

Description GW3965 HCl is a potent, selective LXR agonist for hLXRα and hLXRβ with EC50 of 190 and 30 nM in cell-free assays, respectively.
Targets
hLXRβ [1]
(Cell-free assay)
LXRα/SRC1 LiSA [1]
(Cell-free assay)
hLXRα [1]
(Cell-free assay)
30 nM(EC50) 125 nM(EC50) 190 nM(EC50)
In vitro

GW3965 recruits the steroid receptor coactivator 1 to human LXRα with EC50 of 125 nM in a cell-free ligand-sensing assay. [1] GW3965 shows a potent antagonistic activity against hLXRα and hLXRβ in cell-based assays with EC50 of 190 nM and 30 nM, respectively. Besides, GW3965 also sows excellent selectivity over other nuclear receptors. [1] In human islets, GW3965 (1 μM) reduces expression of selected pro-inflammatory cytokines including IL-8, monocyte chemotactic protein-1 and tissue factor. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
THP1 cells M3HrSmZ2dmO2aX;uJIF{e2G7 NEjPOlcyQCCq M{fkV2lv\HWldHnvckBw\iClaH;s[ZN1\XKxbDDl[oZtfXhiaX6gWGhROSClZXzsd{Bi\nSncjCxPEBpenNuIFXDOVA:OC5yMTFOwG0> M3HEXlE4PDF4NUKx
COS7 cells M{XLV2Z2dmO2aX;uJIF{e2G7 MorLRYN1cX[jdHnvckBw\iCOWGLi[ZRiKGOxLYTyZY5{\mWldHXkJIlvKEORU{egZ4VtdHNid3n0bEBTYFKjbIDoZUBjgSC{ZYDvdpRmeiC2cnHud4FkfGm4YYTpc44h[XO|YYmsJGVEPTB;MD6wNVUh|ryP M{\TclE4PDF4NUKx
human THP1 cells MoDYSpVv[3Srb36gZZN{[Xl? MYe2JIg> MmfuRY51cWmwZnzhcY1ifG:{eTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFSKUEGgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCOUGOtd5RqdXWuYYTl[EBKVDZicILv[JVkfGmxbjDh[pRmeiB4IHjyd{BjgSCHTFnTRUwhUUN3ME2wMlAzKM7:TR?= M2rUPFE5QDByN{[3
mouse RAW264.7 cells MlvRSpVv[3Srb36gZZN{[Xl? MXeyOEBp MXHJcoR2[3Srb36gc4YhYzOKXXPoc4xme3Sncn;sJIVn\my3eDDpckBud3W|ZTDSRXczPjRwNzDj[YxteyCub3Hk[YQhf2m2aDDhZ4V1gWyjdHXkMWxFVCCjZoTldkAzPCCqcoOsJGVEPTB;MD6wNlkh|ryP MoLZNVk4OTd|MES=
human SH-SY5Y cells M1TyV2Z2dmO2aX;uJIF{e2G7 NYXLR4RmOjRiaB?= M4XvZmFod26rc4SgZYN1cX[rdImgZZQhcHWvYX6gUHhT[mW2YTDlfJBz\XO|ZXSgbY4hcHWvYX6gV2guW1l3WTDj[YxteyClbz30doFve2[nY4Tl[EB4cXSqIFfhcFQuVEKGIHHmeIVzKDJ2IHjyd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGVEPTB;MD6xN{DPxE1? MoDiNVkzPjR2OEG=
human HepG2 cells MYrGeY5kfGmxbjDhd5NigQ>? NVPYV2FYTW[oZXP0JI9vKFOURVLQNYMh\2WwZTDlfJBz\XO|aX;uJIlvKGi3bXHuJGhmeEd{IHPlcIx{NCCHQ{WwQVAvOjFizszN MYSxPFk4OzJ6OB?=
human HuH7 cells MlvWSpVv[3Srb36gZZN{[Xl? M4[3O2Fod26rc4SgZYN1cX[rdImgZZQhcHWvYX6gdoVkd22kaX7hcpQhVFiUYnX0ZUBtcWejbnSgZolv\GmwZzDkc41icW5iaX6gbJVu[W5iSIXIO{Bk\WyuczDjc{11emGwc3\lZ5Rm\CC5aYToJIZ2e2WmIFfhcFQuTEKGIHL5JJRz[W6|YXP0bZZifGmxbjDhd5NigSxiRVO1NF0xNjNzIN88US=> MY[xPFk4OzJ6OB?=
CHO cells NHfIVGxHfW6ldHnvckBie3OjeR?= NWfDU4txSWexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBNYFJiYnX0ZUBz\WOncITvdkBmgHC{ZYPz[YQhcW5iQ1jPJINmdGy|IHL5JJJmeG:{dHXyJIF{e2G7LDDFR|UxRTBwNEGg{txO MnzhNVcxOzRzMUm=
CHOK1 cells M1zRXGZ2dmO2aX;uJIF{e2G7 M4\ZbVI1KGh? NW\PSllNSWexbnnzeEBi[3Srdnn0fUBifCCJYXy0MZRi\2enZDDMXHJj\XSjIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJGNJV0tzIHPlcIx{KGGodHXyJFI1KGi{czDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFXDOVA:OC52MjFOwG0> MWqyOVY4PzZ4NB?=
human primary hepatocytes MkfkSpVv[3Srb36gZZN{[Xl? M2\IcVEh|ryP MYnJcoR2[3Srb36gc44hTkGVIHflcoUh\XiycnXzd4lwdiCrbjDoeY1idiCycnntZZJ6KGincHH0c4N6fGW|IHH0JFEhfU1? M2C4WFE4PjZ3OEm3
human HeLa cells MUPGeY5kfGmxbjDhd5NigQ>? M2PIXlEh|ryP M{j6[Wlv\HWldHnvckBw\iCOWGLi[ZRiKFOXTV;5cIF1cW:wIHL5JHNWVU9{IHnuJIh2dWGwIFjlUIEh[2WubIOgZZQhOSC3TTDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? MkTyNVg5ODB5Nke=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Skp2 / pEGFR / EGFR / pERK / ERK ; 

PubMed: 25184494     


GW3965 treatment downregulates SKP2 and EGFR protein levels in BxPC-3 and MIA-PaCa-2 cells. Downregulation of EGFR was concomitant with a downregulation of its own phosphorylation in BxPC-3 and MIA-PaCa-2 at 5 uM GW 3965. ERK1/2 and its phosphorylation were not statistically different in any of the cell lines.

LXRα / LXRβ / ABCA1 / ABCG1; 

PubMed: 11604492     


Differentiated THP-1 macrophages were incubated for 48 h in RPMI medium plus 10% LPDS, Oxysterols [20(S)HC, 22(R)HC, or 22(S)HC, 2.0 μg/ml], synthetic LXR ligand (GW3965 or T1317, 0.1 to 10.0 μM), or RXR ligand (LG268, 50 nM).

25184494 11604492
Immunofluorescence
LAMP-1 / LDLR; 

PubMed: 23382078     


HeLa cells were cultured in 10% LPDS medium for 8 h and then treated with GW3965 (1 μM) for the indicated times. Cells were immunostained with LDLR and LAMP-1 antibodies. Nuclei were counterstained with DAPI (blue). Representative confocal images are shown. T, time; O/N, overnight.

pRelA ; 

PubMed: 26635040     


Freshly isolated PDC (plasmacytoid dendritic cells) were treated for 24 h with 1 mM of GW3965 (GW), followed by TLR7 ligand, R848 (1 mg/mL) for 45 min. Phosphorylation of the NF-κB p65 (pRelA) subunit and its cellular localization were evaluated by confocal microscopy analysis. Results from a representative experiment out of 3 using PDC from 3 different donors.

23382078 26635040
Growth inhibition assay
Cell viability; 

PubMed: 25184494     


A, B, C, PDAC cells (BxPC-3, Mia-PaCa-2, and PANC-1 cell lines, respectively) show dose-dependent decreases in cell proliferation upon treatment with increasing GW3965 concentrations. EC50 calculations indicate that BxPC-3 and Mia-PaCa-2 cells are more sensitive to ligand treatment than PANC-1 cells. 

25184494
In vivo In mice, GW3965 at a dose of 10 mg/kg upregulates ABCA1 expression 8-fold and raises circulating levels of HDL by 30% with Cmax of 12.7 μg/mL and t1/2 of 2 hours. [1] GW3965 (10mg/kg) induces expression of ABCA1 and ABCG1 and shows potent antiatherogenic activity in both LDLR−/− and apoE−/− mice. [2] In male sprague-dawley rats, GW3965 reduces Ang II-mediated increases in blood pressure and decreases vascular Ang II receptor gene expression. [3] In Glioblastoma mouse model, GW3965 results in inducible degrader of LDLR-mediated LDLR degradation, increased expression of the ABCA1 cholesterol efflux transporter, and thus potently promotes tumor cell death. [5]

Protocol

Animal Research:[1]
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  • Animal Models: C57BL/6 mice
  • Dosages: ≤10 mg/kg
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 16 mg/mL warmed (25.86 mM)
Water Insoluble
Ethanol Insoluble

* 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 618.51
Formula

C33H31ClF3NO3.HCl

CAS No. 405911-17-3
Storage powder
in solvent
Synonyms N/A
Smiles C1=CC=C(C=C1)C(CN(CCCOC2=CC=CC(=C2)CC(=O)O)CC3=C(C(=CC=C3)C(F)(F)F)Cl)C4=CC=CC=C4.Cl

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

  • Question 1:

    How to formulate the compound for mouse in vivo experiment?

  • Answer:

    S2630 GW3965 HCl can be dissolved in 2% DMSO/30% PEG 300/dd H2O at 10 mg/mL as a homogeneous suspension. This vehicle is suitable for oral gavage to mice.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID