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GW 3965

GW 3965 is a synthetic ligand that acts as a selective agonist for the liver X receptor (LXR) family of nuclear receptors.
LXRs play a pivotal role in regulating cholesterol, lipid, and glucose homeostasis, making GW 3965 a valuable tool for investigating these pathways.
Expierence the power of PubCompare.ai to optimize your GW 3965 research by easily locating relevant protocols from literature, preprints, and patents, and leveraging AI-driven comparisons to identify the best products and procedures for your needs.

Most cited protocols related to «GW 3965»

1
Mobilizing Hematopoietic Stem Cells
Cited 20 times

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Publication 2013
AMD 3100 Biological Assay BLOOD Cells Chemokine Clodronate Flow Cytometry GW 3965 Immunofluorescence Liposomes Mice, House Saline Solution Sulfoxide, Dimethyl Tissues
2
Transcriptional Regulation Analysis Protocol
Cited 6 times
Two-sided Student’s t-tests were performed to assign significance for cellular phenotypic assays and metabolite levels. Only reproducible binding sites identified by replicate ChIP-seq experiments were reported and used for downstream analyses. ChIP-seq peaks were identified using MACS peak caller [51 ], while motif analysis was performed using MEME [52 (link)] on the top 500 most enriched binding sites. For normalized ChIP-seq read-depth analyses, the number of reads were tabulated across binding site coordinates and normalized to the total number of aligned reads obtained for each ChIP-seq experiment. For mapping reads, we utilized a 100-bp sequence centered on the peak summit of each binding site. For ranking temporal changes in read depth, we generated a linear model comparing replicate ChIP-seq read enrichment values between two time points. Sites with altered enrichment were subsequently divided by slope and p value ranked. The top 50 % of p value-ranked sites from each category were used for cofactor motif analyses. For assigning TF motif fold enrichments, we compared the total number of motifs found across a set of binding sites with the number of motifs identified after scrambling binding site sequences. For RNAP2 read depth promoter analyses, sequences within 500 bp of transcription start sites were used as promoters. Connectivity maps were generated using Cytoscape (http://www.cytoscape.org/) and Enrichment map [53 (link)]. Kyoto Encyclopedia of Genes and Genomes (KEGG) gene pathway enrichments were generated using Gene Set Enrichment Analysis (GSEA; http://software.broadinstitute.org/gsea/msigdb/annotate.jsp). Wilcoxon rank sum tests were used to assign significance for H3K36me3 enrichment analyses. Differential gene expression was determined using DESeq [54 (link)]. High-confidence GW3965 + T0901317 responsive genes were assigned for all targets that passed significance and fold change cutoffs across both drug treatments. For comparison of gene expression with RNAP2 and H3K36me3 occupancy, if a gene harbored multiple promoters and/or transcripts, the promoter and/or gene body coordinate exhibiting the strongest read enrichment was used.
Savic D., Ramaker R.C., Roberts B.S., Dean E.C., Burwell T.C., Meadows S.K., Cooper S.J., Garabedian M.J., Gertz J, & Myers R.M. (2016). Distinct gene regulatory programs define the inhibitory effects of liver X receptors and PPARG on cancer cell proliferation. Genome Medicine, 8, 74.
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Publication 2016
Binding Sites Biological Assay Cells Chromatin Immunoprecipitation Sequencing DNA Replication Gene Expression Genes Genome GW 3965 Human Body Microtubule-Associated Proteins Pharmaceutical Preparations Phenotype Student T0901317 Transcription Initiation Site
3
Cardioprotective Effects of LXR Agonists in Acute Myocardial Infarction
Cited 6 times
This investigation conformed to the National Institutes of Health Guidelines on the Use of Laboratory Animals, and was approved by the Institute’s Animal Ethics Committee. Experiments were performed on wild type (WT) C57BL/6 and LXR-deficient [LXRα-, LXRβ-, or LXRα/β double-knockout (KO)] male mice. Pharmacologic experiments employed LXR endogenous agonist 22(R)-hydroxycholesterol [22(R)-HC] and synthetic agonist GW3965.14 (link), 15 (link) In the acute MI/R protocol, reperfusion commenced for 24 hours following 30 minutes of ischemia. Mice were randomly assigned to the following groups: sham, vehicle, 22(R)-HC (20 mg/kg), or GW3965 (20 mg/kg) by intraperitoneal injection (IP) 15 minutes before reperfusion. To observe the long-term cardioprotective effect of LXRα/β dual agonists, mice were randomly assigned to one of the following groups: sham, vehicle, 22(R)-HC (20 mg/kg), or GW3965 (20 mg/kg) by IP injection 15 minutes before reperfusion, and daily following reperfusion for 4 weeks. Other experiments were designed for MI/R outcome determination in LXRα-, β-, and α/β double-deficiency mice and their WT littermates. Myocardial apoptosis was determined by terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) technique and cardiac caspase-3 activity. Myocardial infarct size was determined by Evans blue-TTC double staining methods.16 (link) In-vivo cardiac function was determined by echocardiography.17 (link) Viable myocardium was assessed via micro-positron emission tomography/computed tomography (micro-PET/CT) scanning. Myocardial reactive oxygen species generation was measured by confocal microscopy via in-situ dehydroetidium (DHE) stain or lucigenin-enhanced chemiluminescence. Myocardial nitrative stress was assessed by nitrotyrosine content. In-vivo knockdown of cardiac-specific LXRα or LXRβ expression was achieved by intramyocardial delivery of siRNA. In-vivo cardiac gene overexpression was achieved by adenoviral-encoded LXRα or LXRβ transfection. An expanded Methods appears in the Data Supplement.
He Q., Pu J., Yuan A., Lau W.B., Gao E., Koch W.J., Ma X.L, & He B. (2014). Activation of LXRα but not LXRβ Protects Against Myocardial Ischemia/Reperfusion Injury. Circulation. Heart failure, 7(6), 1032-1041.
Publication 2014
3-nitrotyrosine Adenoviruses agonists Animal Ethics Committees Animals, Laboratory Apoptosis Caspase 3 Chemiluminescence deoxyuridine triphosphate Dietary Supplements DNA Nucleotidylexotransferase Echocardiography Evans Blue Genes GW 3965 Heart Hydroxycholesterols Injections, Intraperitoneal Ischemia Longterm Effects Lucigenin Males Mice, House Microscopy, Confocal Myocardial Infarction Myocardium Obstetric Delivery Reactive Oxygen Species Reperfusion RNA, Small Interfering Scan, CT PET Stains Transfection
4
Macrophage Culture and Ligand Treatments
Cited 6 times

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Publication 2012
Cells Cholesterol compactin Desmosterol GW 3965 Ligands Lipids Macrophage Mus palmitoleic acid Repression, Psychology Thioglycolates TNF protein, human Triparanol
5
Macrophage Isolation and Manipulation
Cited 5 times
Primary peritoneal macrophages were obtained from thioglycollate-treated mice 4 days after injection. For bone marrow-derived macrophages, bone marrow was isolated from femurs and tibias, and differentiated in DMEM supplemented with 20% fetal bovine serum (FBS), 30% L929 conditioned medium and antibiotics for 6–7 days. MEFs were immortalized by the SV40 Large T antigen retrovirus and selected with puromycin. Immortalized bone marrow-derived macrophages were obtained as previously described (Blasi et al., 1985 (link); Gandino and Varesio, 1990 (link)). To reconstitute immortalized bone marrow derived macrophages from LXR-deficient mice with LXR wild-type or mutants, retrovirus supernatants from Phoenix E cells transfected with the expression vectors were infected to immortalized macrophages. The iBMDM stably expressing wild-type LXRα, LXRβ or mutants were obtained by 300 µg/ml of hygromycin B (Invitrogen). For RNAi experiments in macrophages, cells were transfected with control or ON-TARGETplus SMARTpool siRNAs (25 nM, Dharmacon) targeted RXRα, RXRβ, Ubc9, Hdac4, ABCA1, ABCG1 and TRAF6 using Darmafect 4 (Dharmacon). Cells were used for experiments after 48 hr incubation and target gene knockdown was validated by real-time PCR and Western Blot. For macrophage inflammatory responses, cells were placed in DMEM containing 0.5% FBS, 5 μM simvastatin, 100 μM mevalonic acid and 1 μM GW3965 or DMSO overnight. Cells were then stimulated with 10 ng/ml LPS or vehicle. For cellular cholesterol modification, bone marrow-derived macrophages were placed in DMEM containing 0.5% FBS, 5 μM simvastatin plus 100 μM mevalonic acid for 4 hr, then incubated with complexes of randomly methylated cyclodextrin (Trappsol) and cholesterol (Sigma–Aldrich) (CD/Chol, 100 μM) to overload with cholesterol (Klein et al., 1995 (link)) or hydroxypropyl-β-cyclodextrin (Trappsol) (CD, 10 mM) to deplete cholesterol for 1 hr and stimulated with LPS (10 ng/ml) for 4 hr.
Ito A., Hong C., Rong X., Zhu X., Tarling E.J., Hedde P.N., Gratton E., Parks J, & Tontonoz P. (2015). LXRs link metabolism to inflammation through Abca1-dependent regulation of membrane composition and TLR signaling. eLife, 4, e08009.
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Publication 2015
ABCA1 protein, human ABCG1 protein, human Antibiotics Bone Marrow Cells Cholesterol Cloning Vectors Culture Media, Conditioned Cyclodextrins Femur Fetal Bovine Serum Gene Knockdown Techniques GW 3965 Hygromycin B Hypromellose Inflammation Large T-Antigen Macrophage Macrophages, Peritoneal Mevalonic Acid Mus Puromycin Real-Time Polymerase Chain Reaction Retroviridae RNA, Small Interfering RNA Interference Simian virus 40 Simvastatin simvastatin acid Sulfoxide, Dimethyl Thioglycolates Tibia TNF Receptor Associated Factor 6 Western Blot

Most recents protocols related to «GW 3965»

1
LXR Agonist Inhibits Breast Cancer Growth
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Example 23

We have demonstrated that LXR agonists inhibit in vitro cancer progression phenotypes in breast cancer, pancreatic cancer, and renal cancer. To investigate if LXR agonist treatment inhibits breast cancer primary tumor growth in vivo, mice injected with MDA-468 human breast cancer cells were treated with either a control diet or a diet supplemented with LXR agonist GW3965 2 (FIG. 36).

To determine the effect of orally delivered GW3965 2 on breast cancer tumor growth, 2×106 MDA-468 human breast cancer cells were resuspended in 50 μL PBS and 50 μL matrigel and the cell suspension was injected into both lower memory fat pads of 7-week-old Nod Scid gamma female mice. The mice were assigned to a control diet treatment or a GW3965-supplemented diet treatment (75 mg/kg/day) two days prior to injection of the cancer cells. The GW3965 2 drug compound was formulated in the mouse chow by Research Diets, Inc. Tumor dimensions were measured using digital calipers, and tumor volume was calculated as (small diameter)2×(large diameter)/2.

Treatment with GW3965 resulted in significant reduction in breast cancer tumor size in vivo (FIG. 36).

US11865094B2. Treatment and diagnosis of melanoma (2024-01-09). The Rockefeller University [US]. Inventors: Sohail Tavazoie [US], Nora Pencheva [US].
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Patent 2024
agonists Breast Carcinoma Breast Neoplasm Cancer of Kidney Cardiac Arrest Cells Diet Disease Progression Drug Compounding Fingers Gamma Rays GW 3965 Malignant Neoplasm of Breast Malignant Neoplasms Mammary Carcinoma, Human matrigel Memory Mice, Inbred NOD Mus Neoplasms Pad, Fat Pancreatic Cancer Phenotype SCID Mice Woman
2
LXR Agonist Inhibits Melanoma Metastasis
Not available on PMC !

Example 11

Small molecule agonists of the Liver X Receptor (LXR) have previously been shown to increase Apo E levels. To investigate whether increasing Apo-E levels via LXR activation resulted in therapeutic benefit, assays were carried out to assess the effect of the LXR agonist GW3965 [chemical name: 3-[3-[N-(2-Chloro-3-trifluoromethylbenzyl)-(2,2-diphenylethyl)amino]propyloxy]phenylacetic acid hydrochloride) on Apo-E levels, tumor cell invasion, endothelial recruitment, and in vivo melanoma metastasis (FIG. 10). Incubation of parental MeWo cells in the presence of therapeutic concentrations of GW3965 increased expression of ApoE and DNAJA4 (FIGS. 10A and 10B). Pre-treatment of MeWO cells with GW3965 decreased tumor cell invasion (FIG. 10C) and endothelial recruitment (FIG. 10D). To test whether GW3965 could inhibit metastasis in vivo, mice were administered a grain-based chow diet containing GW3965 (20 mg/kg) or a control diet, and lung metastasis was assayed using bioluminescence after tail-vein injection of 4×104 parental MeWo cells into the mice (FIG. 10E). Oral administration of GW3965 to the mice in this fashion resulted in a significant reduction in in vivo melanoma metastasis (FIG. 10E).

US11865094B2. Treatment and diagnosis of melanoma (2024-01-09). The Rockefeller University [US]. Inventors: Sohail Tavazoie [US], Nora Pencheva [US].
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Patent 2024
Administration, Oral agonists Apolipoproteins E Cardiac Arrest Cells Cereals Diet Endothelium GW 3965 Liver X Receptors Lung Malignant Neoplasms Melanoma Mus Neoplasm Invasiveness Neoplasm Metastasis Parent phenylacetic acid Tail Veins
3
Immune Response Analysis in Mice
For immunization studies, mice were subcutaneously immunized with 50 µg KLH (Sigma-Aldrich) or 100 µg NP-OVA (Biosearch Technologies) emulsified in CFA (Sigma-Aldrich), and lymphoid cells from the draining LNs were stained and analyzed by flow cytometry on day 8 to 10. For viral infection experiments, mice were intraperitoneally injected with LCMV-Armstrong (2 × 105 pfu), and lymphoid cells in the spleen were analyzed on day 8. In some experiments, mice were intraperitoneally treated with either Dimethyl sulfoxide (DMSO) vehicle or 20 mg/kg GW3965 (Tocris).
For BM chimera studies, 8- to 10-wk-old sublethally-irradiated Rag1−/− mice (9 Gy; X-RAD IR160, Precision X-Ray, USA) were i.v. injected 1:1 mixture of WT and Nr1h2−/− BM cells before 6 wk of reconstitution. The recipients were s.c. immunized with KLH in CFA or infected with LCMV, and lymphoid cells from the draining LNs or spleen were analyzed as indicated (46 (link)).
For OT-II T cell cotransfer studies, 1:1 mixture of flow-sorted WT and Nr1h2−/− naïve OT-II T cells (2 × 106 cells) were i.v. transferred into sex-matched B6.SJL congenic recipient mice. One day later, the recipients were s.c. injected with 100 µg OVA (Sigma-Aldrich) emulsified in CFA and lymphoid cells from the draining LNs were analyzed on day 8.
Kim J., Lee H., Lee J.E., Choi G., Chung H., Kim D., Park M.J., Gye Y.S., Shin K.S., Kang C.Y., Kwok S.K, & Chung Y. (2023). Liver X receptor controls follicular helper T cell differentiation via repression of TCF-1. Proceedings of the National Academy of Sciences of the United States of America, 120(9), e2213793120.
Publication 2023
Cells Chimera Flow Cytometry GW 3965 Lymphocytic choriomeningitis virus Lymphoid Cells Mice, Congenic Mus Radiography RAG-1 Gene Spleen Sulfoxide, Dimethyl T-Lymphocyte Vaccination Virus Diseases
4
Isolation and Stimulation of Naïve CD4+ T Cells
CD4+ T cells from the spleen and peripheral LNs were positively selected with CD4 microbeads (L3T4; Miltenyi Biotec), and naive CD4+ T cells were further sorted as CD4+CD25−CD62LhighCD44low cells with the FACSAria III cell sorter (Becton, Dickinson and Company (BD) Biosciences) and stimulated with plate-coated anti-CD3 (1 μg/mL, 145-2C11: BioXCell) and soluble anti-CD28 (1 μg/mL, 37.51; BioXCell) for 3 d in RPMI 1640 (Sigma-Aldrich) supplemented with 10% FBS (Sigma-Aldrich). To measure TCR-mediate protein phosphorylation, flow-sorted naïve CD4+ T cells were stimulated with plate-coated anti-CD3 and anti-CD28 (2 μg/mL) before being analyzed at indicated time points. In some experiments, cells were treated with either DMSO vehicle or 1 µM GW3965 (Tocris), 1 µM BIO (Sigma-Aldrich), or mevalonic acid (Sigma-Aldrich).
Kim J., Lee H., Lee J.E., Choi G., Chung H., Kim D., Park M.J., Gye Y.S., Shin K.S., Kang C.Y., Kwok S.K, & Chung Y. (2023). Liver X receptor controls follicular helper T cell differentiation via repression of TCF-1. Proceedings of the National Academy of Sciences of the United States of America, 120(9), e2213793120.
Publication 2023
CD4 Positive T Lymphocytes Cells GW 3965 IL2RA protein, human Mevalonic Acid Microspheres Muromonab-CD3 Phosphorylation Proteins Spleen Sulfoxide, Dimethyl
5
Synthesis and Characterization of Novel LXR Ligand
Novel LXR ligand GAC0001E5 was synthesized by Otavachemicals, Concord, ON, Canada. Synthetic LXR agonist GW3965 and glutaminase inhibitor BPTES were obtained from Cayman Chemical, Ann Arbor, MI, USA. All cell culture media and FBS were purchased from Thermo Fisher Scientific Inc., Waltham, MA, USA. MCF-7 and MDA-MB-231 cell lines were purchased from the American Type Culture Collection (ATCC), Manassas, VA, USA. A Tamoxifen-resistant MCF-7-TamR cell line was obtained from the Bawa-Khalfe Lab. MCF-7 cells were treated with 1 μM of 4-Hydroxytamoxifen (Selleckchem, Houston, TX, USA) for six months for acquisition of resistance to produce MCF-7-TamR. Furthermore, they were supplemented with 1 μM of 4-Hydroxytamoxifen to maintain resistance [18 (link)]. MCF-7 and MCF-7-TamR cell lines were cultured in DMEM media (Gibco #12430054). MDA-MB-231 cells were cultured in DMEM/F12 (Ham) (Gibco #11330032). Each media type was supplemented with 10% FBS (Gibco #26140079). Cell cultures were maintained in a humidified atmosphere of 5% CO2 at 37 °C.
Premaratne A., Ho C., Basu S., Khan A.F., Bawa-Khalfe T, & Lin C.Y. (2023). Liver X Receptor Inverse Agonist GAC0001E5 Impedes Glutaminolysis and Disrupts Redox Homeostasis in Breast Cancer Cells. Biomolecules, 13(2), 345.
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Publication 2023
Atmosphere Caimans Cell Culture Techniques Cells Culture Media Glutaminase GW 3965 hydroxytamoxifen Ligands MCF-7 Cells MDA-MB-231 Cells Tamoxifen

Top products related to «GW 3965»

1
Gw3965 by Merck Group
Sourced in United States
GW3965 is a synthetic ligand for the liver X receptor (LXR) that can be used in laboratory research applications. It functions as an agonist for the LXR nuclear receptor. The core function of GW3965 is to activate LXR and regulate the expression of LXR target genes.
2
Gw3965 by Cayman Chemical
Sourced in United States
GW3965 is a synthetic ligand for the liver X receptor (LXR) that can be used in research applications. It functions as an agonist to activate LXR, a transcription factor involved in the regulation of cholesterol and lipid homeostasis.
3
Gw3965 by Bio-Techne
Sourced in United Kingdom, United States
GW3965 is a synthetic ligand that acts as an agonist for the liver X receptor (LXR). LXRs are nuclear receptors that play a role in the regulation of cholesterol, fatty acid, and glucose homeostasis.
4
Fetal bovine serum (fbs) by Thermo Fisher Scientific
Sourced in United States, China, United Kingdom, Germany, Australia, Japan, Canada, Italy, France, Switzerland, New Zealand, Brazil, Belgium, India, Spain, Israel, Austria, Poland, Ireland, Sweden, Macao, Netherlands, Denmark, Cameroon, Singapore, Portugal, Argentina, Holy See (Vatican City State), Morocco, Uruguay, Mexico, Thailand, Sao Tome and Principe, Hungary, Panama, Hong Kong, Norway, United Arab Emirates, Czechia, Russian Federation, Chile, Moldova, Republic of, Gabon, Palestine, State of, Saudi Arabia, Senegal
Fetal Bovine Serum (FBS) is a cell culture supplement derived from the blood of bovine fetuses. FBS provides a source of proteins, growth factors, and other components that support the growth and maintenance of various cell types in in vitro cell culture applications.
5
Gw3965 by Selleck Chemicals
Sourced in United States
GW3965 is a synthetic agonist of the liver X receptor (LXR) transcription factor. It functions by activating LXR, which is involved in the regulation of genes related to cholesterol and lipid metabolism.
6
T0901317 by Cayman Chemical
Sourced in United States
T0901317 is a synthetic small molecule that functions as an agonist for the liver X receptor (LXR) family of nuclear receptors. This compound is commonly used in scientific research to study the biological effects mediated by LXR activation.
7
Lipopolysaccharides (lps) by Merck Group
Sourced in United States, Germany, China, United Kingdom, Sao Tome and Principe, Macao, Italy, Japan, Canada, France, Switzerland, Israel, Australia, Spain, India, Ireland, Brazil, Poland, Netherlands, Sweden, Denmark, Hungary, Austria, Mongolia
The LPS laboratory equipment is a high-precision device used for various applications in scientific research and laboratory settings. It is designed to accurately measure and monitor specific parameters essential for various experimental procedures. The core function of the LPS is to provide reliable and consistent data collection, ensuring the integrity of research results. No further details or interpretations can be provided while maintaining an unbiased and factual approach.
8
Penicillin by Thermo Fisher Scientific
Sourced in United States, United Kingdom, Germany, China, France, Canada, Japan, Australia, Switzerland, Italy, Israel, Belgium, Austria, Spain, Brazil, Netherlands, Gabon, Denmark, Poland, Ireland, New Zealand, Sweden, Argentina, India, Macao, Uruguay, Portugal, Holy See (Vatican City State), Czechia, Singapore, Panama, Thailand, Moldova, Republic of, Finland, Morocco
Penicillin is a type of antibiotic used in laboratory settings. It is a broad-spectrum antimicrobial agent effective against a variety of bacteria. Penicillin functions by disrupting the bacterial cell wall, leading to cell death.
9
Streptomycin by Thermo Fisher Scientific
Sourced in United States, United Kingdom, Germany, China, France, Canada, Australia, Japan, Switzerland, Italy, Belgium, Israel, Austria, Spain, Netherlands, Poland, Brazil, Denmark, Argentina, Sweden, New Zealand, Ireland, India, Gabon, Macao, Portugal, Czechia, Singapore, Norway, Thailand, Uruguay, Moldova, Republic of, Finland, Panama
Streptomycin is a broad-spectrum antibiotic used in laboratory settings. It functions as a protein synthesis inhibitor, targeting the 30S subunit of bacterial ribosomes, which plays a crucial role in the translation of genetic information into proteins. Streptomycin is commonly used in microbiological research and applications that require selective inhibition of bacterial growth.
10
T0901317 by Merck Group
Sourced in United States, Japan, Germany
T0901317 is a selective agonist of the liver X receptor (LXR) family of nuclear receptors. It acts as a modulator of gene transcription involved in cholesterol, fatty acid, and glucose metabolism. The core function of T0901317 is to serve as a research tool for studying the role of LXR in biological processes.

More about "GW 3965"

Explore the versatility of GW 3965, a powerful synthetic ligand that selectively targets the liver X receptor (LXR) family of nuclear receptors.
LXRs play a crucial role in regulating cholesterol, lipid, and glucose homeostasis, making GW 3965 an invaluable tool for investigating these critical biological pathways.
Unlock the full potential of your GW 3965 research with the help of PubCompare.ai, the leading AI-driven platform for enhancing reproducibility and accuracy.
Easily locate relevant protocols from literature, preprints, and patents, and leverage the power of AI-driven comparisons to identify the best products and procedures for your needs.
Discover how GW 3965 can be used in combination with other key compounds, such as the LXR agonist T0901317, the bacterial endotoxin lipopolysaccharide (LPS), and the antibiotic mixture of penicillin and streptomycin, to uncover the intricate mechanisms underlying lipid and glucose regulation.
Expierence the transformative impact of PubCompare.ai and take your GW 3965 research to new heights of efficiency and effectiveness.