GW3965 HCl

Catalog No.S2630

GW3965 HCl Chemical Structure

Molecular Weight(MW): 618.51

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

Size Price Stock Quantity  
In DMSO USD 240 In stock
USD 97 In stock
USD 150 In stock
USD 570 In stock
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Cited by 11 Publications

6 Customer Reviews

  • The interaction of liver X receptor a (LXRa) and b-catenin is involved in oxLDL regulation of DKK1. Western blot analysis of cells pretreated with DMSO or GW3965 (1 μM).

    FEBS Lett, 2015, 589(1):52-8.. GW3965 HCl purchased from Selleck.

    a. Western blot analysis for EpCAM, PKM2, and CK19 expression in livers from C57BL/6J mice treated with DDC for 1 week in the absence or presence of GW3965 (10 mg/kg; n = 4 per group). *P < 0.05, **P < 0.01. c Western blot analysis of p-STAT3, t-STAT3, and SOCS3 in WB-F344 cells treated with GW3965 (5 μM) or DMSO as control in response to IL-6 (50 ng/ml) treatment for 0, 0.25, 0.5, 0.75, 1, and 2 h.

    Arch Toxicol, 2017, 91(1):271-287. GW3965 HCl purchased from Selleck.

  • GW3965 increased neural progenitor cell (NPC) proliferation concentration-dependently in vitro. (A) The purity of neural progenitor cell (NPC) was determined by immunocytochemistry staining with nestin, a marker of NPC, was labeled in red, and the nucleus was labeled in blue. (B–F) The NPCs were treated with GW3965 (0, 1, 10, 100 μM) for 3 d and subjected to BrdU staining after incorporation for 4 h before fixing, neurosphere initiation medium (NPIM) served as a positive control. (G) Proliferating NPCs showed BrdU positive labeled in green. The statistical values of each group. n=6 wells from three independent experiments. *P < 0.05, **P < 0.01 compared with control, scale bar=100 μm. (For interpretation of the references to color in this figure legend, the reader is referred to the web version of this article.)

    Exp Neurol, 2018, 304:21-29. GW3965 HCl purchased from Selleck.

    Analysis of factor expression in response to LPS + Kavain treatment in cells. To examine whether Kavain affects LITAF translocation via another kinase/factor, a secondary Western Blot was performed. The WT mice macrophages had been untreated or treated with 1 μM GW3965 alone, 5 μM LY294002 alone, or 200 μg/ml Kavain alone as the negative control (lanes 1 or 3–5), or treated with 0.1 μg/ml E. coli LPS alone as the positive control (lane 2), or co‐treated with 0.1 μg/ml LPS + 1 μM GW3965 (lane 6), 0.1 μg/ml LPS + 5 μM LY2940020 (lane 7), or 1 μg/ml LPS + 200 μg/ml Kavain (lane 8) for 1 h. The treated cells’ protein levels or phosphorylation levels were identified by Western Blot, which were then compared to the control (Actin for whole cells protein or Lamin B for nuclear protein). The intensities of each test factor protein (lane 6–8) from LPS alone‐treated cells were assigned to a base value (100%, lane 2). The intensity of the same group from other treatments was calculated relative to this base value after normalization with control (Actin/Lamin B).

    J Cell Biochem, 2016, 117(10):2272-80. GW3965 HCl purchased from Selleck.

  • The effects of GW3965 on NDV infection. (A) The DF-1 cells were cultured with different concentrations of GW3965. Cell viability was determined by MTT assay at 24 h. (B) Synthetic LXR agonist GW3965 inhibited NDV infection in DF-1 cells. Cells were pretreated with GW3965 (1 μM) for 2 h, then infected with NDV (MOI = 1). GW3965 (1 μM) was continuously present during the infection. The expression level of the viral NP protein was determined by western blot. (C) The titers of the supernatant were determined by TCID50. (D) The viral gRNA in cells was detected by qRT-PCR assay.

    Arch Virol, 2016, 161(9):2491-501.. GW3965 HCl purchased from Selleck.

    GW3965 up-regulated the expression of LXRα in glucose-induced H9C2 cells by Western blot analysis.

    Biochem Cell Biol, 2018, 96(1):11-18. GW3965 HCl purchased from Selleck.

Purity & Quality Control

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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 MkjNSpVv[3Srb36gZZN{[Xl? NILTU2syQCCq MnnoTY5lfWO2aX;uJI9nKGOqb3zld5Rmem:uIHXm[ox2gCCrbjDUTHAyKGOnbHzzJIFnfGW{IEG4JIhzeyxiRVO1NF0xNjBzIN88US=> M2jKPFE4PDF4NUKx
COS7 cells M4\wfGZ2dmO2aX;uJIF{e2G7 NIqwfHhC[3SrdnH0bY9vKG:oIFzYVoJmfGFiY3:teJJidnOoZXP0[YQhcW5iQ1;TO{Bk\WyuczD3bZRpKFK[UnHsdIhiKGK7IILldI9zfGW{IITyZY5{[WO2aY\heIlwdiCjc4PhfUwhTUN3ME2wMlAyPSEQvF2= M4nWOlE4PDF4NUKx
human THP1 cells MWfGeY5kfGmxbjDhd5NigQ>? MX[2JIg> M{L0NGFvfGmrbn\sZY1u[XSxcomgZYN1cX[rdImgZYdicW6|dDDoeY1idiCWSGCxJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiTGDTMZN1cW23bHH0[YQhUUx4IIDyc4R2[3Srb36gZYZ1\XJiNjDodpMh[nliRVzJV2EtKEmFNUC9NE4xOiEQvF2= M4SxNFE5QDByN{[3
mouse RAW264.7 cells MVLGeY5kfGmxbjDhd5NigQ>? NGG5R3QzPCCq NIPPcW5KdmS3Y4Tpc44hd2ZiW{PIYYNpd2ync4Tldo9tKGWoZnz1fEBqdiCvb4Xz[UBTSVd{NkSuO{Bk\WyuczDsc4Fl\WRid3n0bEBi[2W2eXzheIVlNUyGTDDh[pRmeiB{NDDodpMtKEWFNUC9NE4xOjlizszN NWr2TXh4OTl5MUezNFQ>
human SH-SY5Y cells NYrvXnY5TnWwY4Tpc44h[XO|YYm= NXPDVo1HOjRiaB?= NHH1copC\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJGxZWmKndHGg[ZhxemW|c3XkJIlvKGi3bXHuJHNJNVO\NWmgZ4VtdHNiY3:teJJidnOoZXP0[YQhf2m2aDDHZYw1NUyERDDh[pRmeiB{NDDodpMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBGSzVyPUCuNVMh|ryP NHnUPGwyQTJ4NES4NS=>
human HepG2 cells MnzpSpVv[3Srb36gZZN{[Xl? MVTF[oZm[3Rib36gV3JGSlBzYzDn[Y5mKGW6cILld5Nqd25iaX6gbJVu[W5iSHXwS|Ih[2WubIOsJGVEPTB;MD6yNUDPxE1? MYixPFk4OzJ6OB?=
human HuH7 cells M{jzfGZ2dmO2aX;uJIF{e2G7 NUe0THkySWexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBz\WOxbXLpcoFvfCCOWGLi[ZRiKGyrZ3Hu[EBjcW6maX7nJIRwdWGrbjDpckBpfW2jbjDIeWg4KGOnbHzzJINwNXS{YX7z[oVkfGWmIIfpeIgh\nW|ZXSgS4FtPC2GQlSgZpkhfHKjboPhZ5RqfmG2aX;uJIF{e2G7LDDFR|UxRTBwM{Gg{txO NUGySXdMOTh7N{OyPFg>
CHO cells NYezOFVDTnWwY4Tpc44h[XO|YYm= M2izOGFod26rc4SgZYN1cX[rdImgZZQhcHWvYX6gUHhTKGKndHGgdoVk\XC2b4Kg[ZhxemW|c3XkJIlvKEOKTzDj[YxteyCkeTDy[ZBwenSncjDhd5NigSxiRVO1NF0xNjRzIN88US=> NIrpfmUyPzB|NEGxPS=>
CHOK1 cells MV7GeY5kfGmxbjDhd5NigQ>? MUGyOEBp MXPB[49vcXO2IHHjeIl3cXS7IHH0JGdidDRvdHHn[4VlKEy[UnLleIEhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iQ1jPT|Eh[2WubIOgZYZ1\XJiMkSgbJJ{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhTUN3ME2wMlQzKM7:TR?= MVyyOVY4PzZ4NB?=
human primary hepatocytes MmfRSpVv[3Srb36gZZN{[Xl? Ml\WNUDPxE1? M3nBcmlv\HWldHnvckBwdiCIQWOg[4Vv\SCneIDy[ZN{cW:wIHnuJIh2dWGwIIDybY1ienliaHXwZZRw[3m2ZYOgZZQhOSC3TR?= MXGxO|Y3PTh7Nx?=
human HeLa cells NET6N3RHfW6ldHnvckBie3OjeR?= NIrWVIUyKM7:TR?= NXq1Z25xUW6mdXP0bY9vKG:oIFzYVoJmfGFiU2XNU5lt[XSrb36gZpkhW1WPT{KgbY4hcHWvYX6gTIVN[SClZXzsd{BifCBzIIXNJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= MWWxPFgxODd4Nx?=

... 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]
+ Expand
  • Animal Models: C57BL/6 mice
  • Formulation: GW3965 is dissolved in 0.5% Methyl Cellulose.
  • 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

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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

Tel: +1-832-582-8158 Ext:3

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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