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Bexarotene

Manufactured by Merck Group
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Bexarotene is a synthetic retinoid compound developed by Merck Group. It functions as a selective agonist of retinoid X receptors (RXRs). Bexarotene is primarily used as a research tool in laboratory settings to study the effects of RXR activation on cellular processes and signaling pathways.

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Lab products found in correlation

Dimethyl sulfoxide (dmso), by Merck Group (4 mentions) 5 fluoro 2 deoxyuridine fudr, by Merck Group (1 mentions) Sb 399885 hydrochloride, by Bio-Techne (1 mentions) Entecavir, by Merck Group (1 mentions) Sulfo nhs lc biotin, by Thermo Fisher Scientific (1 mentions) Tamibarotene, by Merck Group (1 mentions) Magnetic separation column, by Miltenyi Biotec (1 mentions) Sodium pyruvate, by Thermo Fisher Scientific (1 mentions) Bx 912, by Selleck Chemicals (1 mentions) Cd62l mel 14, by BD (1 mentions) Fetal calf serum (fcs), by Atlanta Biologicals (1 mentions) Aktviii, by Santa Cruz Biotechnology (1 mentions) Non essential amino acids (neaa), by Thermo Fisher Scientific (1 mentions) 2 deoxyglucose 2 dg, by Merck Group (1 mentions) Rpmi 1640, by Thermo Fisher Scientific (1 mentions) L glutamine, by Thermo Fisher Scientific (1 mentions) Penicillin streptomycin, by Thermo Fisher Scientific (1 mentions) Anti pe microbeads, by Miltenyi Biotec (1 mentions) Accu check glucometer, by Roche (1 mentions) Triton x, by Merck Group (1 mentions)

17 protocols using bexarotene

1

Sodium Phosphate Fibril Growth Buffer

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Fibril growth buffer was prepared by dissolving sodium phosphate monohydrate (Mallinckrodt) in deionized water to a final concentration of 40 mM and adjusting pH to 7.4 using NaOH. Bexarotene stock solution was prepared by dissolving Bexarotene (Sigma–Aldrich) in dimethyl sulfoxide (Sigma–Aldrich) to a final concentration of 0.2 mM.
Mafimoghaddam S., Xu Y., Sherman M.B., Orlova E.V., Karki P., Orman M.A, & Vekilov P.G. (2022). Suppression of amyloid-β fibril growth by drug-engineered polymorph transformation. The Journal of Biological Chemistry, 298(12), 102662.
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2

ApoE Isoforms and Cholesterol Transport

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ApoA-I and HDL were purchased from VWR (Fontenay-sous-Bois, France). ApoE2 and E4 were purchased from Clinisciences (Montrouge, France) and were resuspended in sterile water at a concentration of 1 mg/mL. Bexarotene, Lucifer Yellow (LY), and human serum albumin (HSA) were purchased from Sigma. Bexarotene was dissolved in DMSO (dimethylsulfoxide from Sigma) at concentration of 40 mM. [ 3 H]cholesterol (43 Ci/mmol), [ 14 C]sucrose (630 mCi/mmol), and [ 3 H]inulin (1.25 Ci/mmol) were purchased from PerkinElmer Life and Analytical Sciences (Waltham, MA, USA). Fluorescent amyloid beta-protein (1-40) (human)-Cy5 labeled was purchased from Phoenix Pharmaceuticals (Strasbourg, France). The powder was reconstituted according to the manufacturer's instructions, in order to avoid peptide aggregation. Briefly, the peptide was resuspended in 10% DMSO in buffer and stored at -20 • C. The ABCB1 inhibitor elacridar was kindly provided by Dr. Stefan Lundquist (AstraZeneca R&D, Södertälje, Sweden) and resuspended in DMSO.
Kuntz M., Candela P., Saint-Pol J., Lamartinière Y., Boucau M.C., Sevin E., Fenart L, & Gosselet F. (2015). Bexarotene Promotes Cholesterol Efflux and Restricts Apical-to-Basolateral Transport of Amyloid-β Peptides in an In Vitro Model of the Human Blood-Brain Barrier. Journal of Alzheimer's disease : JAD, 48(3).
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3

Bexarotene Colloid Formulation Protocol

Cited 1 time
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Bexarotene was obtained from Sigma-Aldrich (St. Louis, MO) at the highest purity available. Colloid formation was performed by first dissolving the Bexarotene power in 10 mM solution stocks of 100% DMSO, before a serial dilution in 20 mM NaP (pH 8.0) and 0.2 mM EDTA to 100 μM in 1% (v/v) DMSO (38 (link)).
Miller A., Chia S., Toprakcioglu Z., Hakala T., Schmid R., Feng Y., Kartanas T., Kamada A., Vendruscolo M., Ruggeri F.S, & Knowles T.P. (2023). Enhanced surface nanoanalytics of transient biomolecular processes. Science Advances, 9(2), eabq3151.
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4

C. elegans Maintenance and Drug Assays

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All chemicals for C. elegans maintenance were bought from Fisher Scientific and Sigma-Aldrich. Drug compounds P7C3 (2 M Biotec), bexarotene (Sigma-Aldrich, lot no: 024M4723 V), and SB 399885 hydrochloride (Tocris, lot no: 2A/148640) were dissolved in DMSO (Sigma-Aldrich, lot no: RNBD6062) at 100 mM and used at four different concentrations in the worm culture as mentioned in the text. 5-Fluoro-2-deoxyuridine (FUdR, Sigma-Aldrich, lot no: SLBL9184 V) was dissolved in water.
Monda S., Hegarty E., Sahn J.J., Scott L.L., Gökçe S.K., Martin C., Ghorashian N., Satarasinghe P.N., Iyer S., Sae-Lee W., Hodges T.R., Pierce J.T., Martin S.F, & Ben-Yakar A. (2018). High-Content Microfluidic Screening Platform Used To Identify σ2R/Tmem97 Binding Ligands that Reduce Age-Dependent Neurodegeneration in C. elegans SC_APP Model. ACS chemical neuroscience, 9(5), 1014-1026.
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5

Biotin Labeling and Retinoid Signaling

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Sulfo-NHS-LC-Biotin (A39257) was purchased from Invitrogen. Myrcludex-B was provided by Dr. Stephan Urban, at the University Hospital Heidelberg. Bexarotene (SML0282), ATRA (R2625), Tamibarotene (T3205), Alitretinoin (R4643), Entecavir, and DMSO were all purchased from Sigma-Aldrich.
Gad S.A., Sugiyama M., Tsuge M., Wakae K., Fukano K., Oshima M., Sureau C., Watanabe N., Kato T., Murayama A., Li Y., Shoji I., Shimotohno K., Chayama K., Muramatsu M., Wakita T., Nozaki T, & Aly H.H. (2022). The kinesin KIF4 mediates HBV/HDV entry through the regulation of surface NTCP localization and can be targeted by RXR agonists in vitro. PLoS Pathogens, 18(3), e1009983.
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6

Murine T Cell Isolation and Expansion

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Complete medium (CM) comprised RPMI-1640 (Gibco, Invitrogen, Carlsbad, CA) supplemented with 10% v/v FCS (Atlanta Biologicals, Lawrenceville, GA), non-essential amino acids, L-glutamine, sodium pyruvate, penicillin-streptomycin and 2-ME (all from Invitrogen, Carlsbad, CA). The mouse CD4-negative isolation kit for T cell isolation and αCD3/αCD28-coated beads (artificial APC, Dynal) for ex-vivo T cell expansion were from Invitrogen. Anti-PE microbeads and magnetic separation columns were from Miltenyi Biotec (Auburn, CA). ATRA, 2-deoxyglucose (2-DG), bexarotene and lithium chloride (LiCl) were from Sigma Aldrich (St. Louis, MO). Mouse rIL-2 and human rTGF-β1 (CHO cell-derived) were from PeproTech (Rocky Hills, NJ), rapamycin was from LC labs (Woburn, MA), the PDK inhibitor BX-912 was from Selleck Chemicals (Houston, TX) and the Akt inhibitor Akt-VIII from Santa Cruz Biotechnology (Dallas, TX). Anti-mouse CD4 (clone L3T4), -Foxp3 (FJK-16s), -CD25 (PC61.5), -CCR9 (eBioCW-1.2), -α4β7/LPAM-1 (DATK32) and -Helios (22F6) Abs were obtained from eBioscience (San Diego, CA). Anti-mouse CD44 (1M7) and -CD62L (MEL-14) were from BD Biosciences (San Diego, CA). Anti-mouse retinoic acid receptor alpha (RARα; EP1823Y) was from Abcam (Cambridge, MA).
Chen L.C., Nicholson Y.T., Rosborough B.R., Thomson A.W, & Raimondi G. (2016). A novel mTORC1-dependent, Akt-independent pathway differentiates the gut tropism of regulatory and conventional CD4 T cells. Journal of immunology (Baltimore, Md. : 1950), 197(4), 1137-1147.
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7

Metabolic Parameter Assessment Protocol

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Includes Accu-check glucometer (Roche Diagnostics, Germany), Ultra-sensitive insulin ELISA kit (Crystal Chem Inc, USA), TAG estimation kit (Diasys Diagnostics system, Germany), FFA estimation kit (Randox Laboratories, UK), Cholesterol estimation kit (Diasys Diagnostics system, Germany, cat# 113009910704), Glycerol estimation kits (Sigma, cat#F6428). Triton-X and Fluromount were procured from Sigma-Aldrich. Bexarotene (Sigma).
Sadasivuni M.K., Reddy B.M., Singh J., Anup M.O., Sunil V., Lakshmi M.N., Yogeshwari S., Chacko S.K., Pooja T.L., Dandu A., Harish C., Gopala A.S., Pratibha S., Naveenkumar B.S., Pallavi P.M., Verma M.K., Moolemath Y., Somesh B.P., Venkataranganna M.V, & Jagannath M.R. (2014). CNX-013-B2, a unique pan tissue acting rexinoid, modulates several nuclear receptors and controls multiple risk factors of the metabolic syndrome without risk of hypertriglyceridemia, hepatomegaly and body weight gain in animal models. Diabetology & Metabolic Syndrome, 6, 83.
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8

Bexarotene Lipid Membrane Interactions

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Bexarotene was purchased from Sigma-Aldrich Chemie GmbH (Deisenhofen, Germany). The lipids 1,2-dihexanoyl-sn-glycero-3-phosphocholine (DHPC), 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC), 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC) as well as the sn-1 chain perdeuterated POPC-d31, 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphoethanolamine (POPE), porcine brain sphingomyelin, bovine heart lipid extract, and cholesterol were purchased from Avanti Polar Lipids, Inc. (Alabaster, Al).
Kamp F., Scheidt H.A., Winkler E., Basset G., Heinel H., Hutchison J.M., LaPointe L.M., Sanders C.R., Steiner H, & Huster D. (2018). Binding of Bexarotene to the Amyloid Precursor Protein Transmembrane Domain in Liposomes Alters its α-Helical Conformation but Inhibits γ-Secretase Non-Selectively. ACS chemical neuroscience, 9(7), 1702-1713.
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9

Preparation of Retinoid Stock Solutions

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ATRA and 13-cis-RA were prepared as stock solutions at a concentration of 100 mM in dimethyl sulfoxide (DMSO; Sigma); 9-cis retinoic acid (9-cis-RA), retinoic acid p-hydroxyanilide (Fenretinide, 4-HPR) and Bexarotene (BEX) were prepared at a concentration of 10 mM in DMSO (all purchased from Sigma Aldrich, St. Louis, MO, USA). Reagents were stored at -20°C under light-free conditions.
Dobrotkova V., Chlapek P., Jezova M., Adamkova K., Mazanek P., Sterba J, & Veselska R. (2019). Prediction of neuroblastoma cell response to treatment with natural or synthetic retinoids using selected protein biomarkers. PLoS ONE, 14(6), e0218269.
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10

Thyroid Cancer Cell Proliferation Assay

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For PPARγ agonist treatments, thyroid cancer cells were treated with 5, 10, 20, or 40 μM rosiglitazone (RGZ) (Sigma-Aldrich, St. Louis, MO) for 24, 48, or 72 hours. For RXR agonist treatment, thyroid cancer cells were treated with 10 nM, 100 nM, 1 μM, or 10 μM bexarotene (Sigma-Aldrich) for 24, 48, or 72 hours. Cell growth and viability were determined by the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay.
Chen J.Y., Wang J.J., Lee H.C., Chi C.W., Lee C.H, & Hsu Y.C. (2020). Combination of peroxisome proliferator–activated receptor gamma and retinoid X receptor agonists induces sodium/iodide symporter expression and inhibits cell growth of human thyroid cancer cells. Journal of the Chinese Medical Association, 83(10), 923-930.
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