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 8 Publications

6 Customer Reviews

  • 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.

  • 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.

    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

Choose Selective Liver X Receptor Inhibitors

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.
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 Mk[xSpVv[3Srb36gZZN{[Xl? NXj1SGl[OThiaB?= NVH2WYpIUW6mdXP0bY9vKG:oIHPoc4xme3Sncn;sJIVn\my3eDDpckBVUFBzIHPlcIx{KGGodHXyJFE5KGi{czygSWM2OD1yLkCxJO69VQ>? MVyxO|QyPjV{MR?=
COS7 cells NVPhPGF[TnWwY4Tpc44h[XO|YYm= MYnBZ5RqfmG2aX;uJI9nKEy[UnLleIEh[29vdILhcpNn\WO2ZXSgbY4hS0:VNzDj[YxteyC5aYToJHJZWmGucHjhJIJ6KHKncH;yeIVzKHS{YX7zZYN1cX[jdHnvckBie3OjeTygSWM2OD1yLkCxOUDPxE1? Mon6NVc1OTZ3MkG=
human THP1 cells Ml\0SpVv[3Srb36gZZN{[Xl? NEXQdGY3KGh? NUPl[FF4SW62aXnu[oxidW2jdH;yfUBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGTIVFEh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDMVHMue3SrbYXsZZRm\CCLTE[gdJJw\HWldHnvckBi\nSncjC2JIhzeyCkeTDFUGlUSSxiSVO1NF0xNjB{IN88US=> NHrYVFcyQDhyMEe2Oy=>
mouse RAW264.7 cells NYT5WHB6TnWwY4Tpc44h[XO|YYm= MV:yOEBp MkL1TY5lfWO2aX;uJI9nKFt|SG3jbI9t\XO2ZYLvcEBm\m[udYigbY4hdW:3c3WgVmFYOjZ2LkegZ4VtdHNibH;h[IVlKHerdHigZYNmfHmuYYTl[E1NTExiYX\0[ZIhOjRiaILzMEBGSzVyPUCuNFI6KM7:TR?= NWLZPHF7OTl5MUezNFQ>
human SH-SY5Y cells MYnGeY5kfGmxbjDhd5NigQ>? MUKyOEBp MYHB[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIFzYVoJmfGFiZYjwdoV{e2WmIHnuJIh2dWGwIGPIMXN[PVliY3XscJMh[29vdILhcpNn\WO2ZXSge4l1cCCJYXy0MWxDTCCjZoTldkAzPCCqcoOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxRTBwMUOg{txO MXixPVI3PDR6MR?=
human HepG2 cells Mo\5SpVv[3Srb36gZZN{[Xl? M3\EfmVn\mWldDDvckBUWkWEUEHjJIdmdmViZYjwdoV{e2mxbjDpckBpfW2jbjDI[ZBIOiClZXzsd{whTUN3ME2wMlIyKM7:TR?= M4HHNFE5QTd|Mki4
human HuH7 cells NYDmUopVTnWwY4Tpc44h[XO|YYm= MnzURYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDy[YNwdWKrbnHueEBNYFKkZYThJIxq\2GwZDDibY5lcW6pIHTvcYFqdiCrbjDoeY1idiCKdVi3JINmdGy|IHPvMZRz[W6|ZnXjeIVlKHerdHig[pV{\WRiR3HsOE1FSkRiYomgeJJidnOjY4TpeoF1cW:wIHHzd4F6NCCHQ{WwQVAvOzFizszN NI\Nd4MyQDl5M{K4PC=>
CHO cells NUTEb3RKTnWwY4Tpc44h[XO|YYm= NV;GVo4xSWexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBNYFJiYnX0ZUBz\WOncITvdkBmgHC{ZYPz[YQhcW5iQ1jPJINmdGy|IHL5JJJmeG:{dHXyJIF{e2G7LDDFR|UxRTBwNEGg{txO MYWxO|A{PDFzOR?=
CHOK1 cells MUjGeY5kfGmxbjDhd5NigQ>? NILi[pczPCCq NF70O4JC\2:waYP0JIFkfGm4aYT5JIF1KEejbESteIFo\2WmIFzYVoJmfGFiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gR2hQUzFiY3XscJMh[W[2ZYKgNlQhcHK|IHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiRVO1NF0xNjR{IN88US=> Mkj4NlU3Pzd4NkS=
human primary hepatocytes NX;2WmxbTnWwY4Tpc44h[XO|YYm= NV\3XHJZOSEQvF2= Mo\GTY5lfWO2aX;uJI9vKE[DUzDn[Y5mKGW6cILld5Nqd25iaX6gbJVu[W5icILpcYFzgSCqZYDheI9kgXSnczDheEAyKHWP M{\xdVE4PjZ3OEm3
human HeLa cells M3yzbGZ2dmO2aX;uJIF{e2G7 MojSNUDPxE1? M4G5dmlv\HWldHnvckBw\iCOWGLi[ZRiKFOXTV;5cIF1cW:wIHL5JHNWVU9{IHnuJIh2dWGwIFjlUIEh[2WubIOgZZQhOSC3TTDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? NVTnXop2OTh6MEC3Olc>

... Click to View More Cell Line Experimental Data

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]


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


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