2. Signaling Pathways
  3. Metabolic Enzyme/Protease
    Vitamin D Related/Nuclear Receptor
  4. RAR/RXR
  5. RXRα Isoform

RXRα

RXRα is a nuclear receptor that regulates transcription through heterodimerization with diverse nuclear receptors, linking retinoid signaling to cell proliferation, differentiation, lipid metabolism, and pharmacology[1]. Mechanistically, RXR-containing heterodimers control liver physiology by modulating lipid and bile acid metabolism in hepatocytes, cholesterol transport in macrophages, and fibrogenesis in hepatic stellate cells[2]. In mouse liver, RXRα binds widely across the genome and supports sex-dimorphic expression of lipid-processing genes, including Scd1, Fasn, Elovl6, and Pnpla3[3]. In disease models, altered RXRα expression or truncated RXRα connects RXRα biology to prostate cancer, chronic myeloid leukemia, and tumor-growth pathways involving PI3K/AKT and NF-κB signaling[4][5][6]. Compared with RXRβ and RXRγ, RXRα belongs to RXR isotypes with distinct properties that modulate RXR-containing heterodimer activity, making isoform selection important in experimental design[1]. For research applications, RXR ligands such as LG268, clinically relevant RXRA ligands, and sulindac analogs provide tools to test RXRα-dependent transcriptional regulation, leukemia drug sensitivity, and truncated RXRα signaling[3][5][6].

RXRα Related Products (13):

Cat. No. Product Name Effect Purity
  • HY-W014589
    2,4-Di-tert-butylphenol
    		Activator 99.97%
    2,4-Di-tert-butylphenol (2,4-DTBP) is an orally active RXRα activator and a human estrogen receptor ligand with anti-inflammatory and antioxidant activities, which can induce apoptosis in tumor cells. 2,4-Di-tert-butylphenol can activate the RXRα subtype in LXRα/RXRα, PPARγ/RXRα, and hormone receptor β/RXRα. 2,4-Di-tert-butylphenol also has antiviral and antifungal activities and has the potential to inhibit Aβ-induced neurotoxicity. 2,4-Di-tert-butylphenol can be used as an intermediate in the preparation of antioxidants and UV stabilizers, and is also used in the manufacture of drugs and fragrances.
  • HY-108531
    ER 50891
    		Antagonist 98.59%
    ER 50891 is a RARα antagonist. ER 50891 can significantly antagonize the inhibitory effect of all-trans retinoic acid (ATRA) on the total cell metabolic activity and proliferation of MC3T3-E1 preosteoblasts. ER 50891 rescues ATRA-inhibited osteocalcin (OCN) expression and extracellular matrix mineralization, and suppresses alkaline phosphatase (ALP) activity synergistically. ER 50891 can be used for the study of osteoporosis related to ATRA-induced inhibition of osteoblastogenesis.
  • HY-163436
    F44-A13
    		Antagonist
    F44-A13 is an orally active and highly selective farnesoid X receptor (FXR) antagonist with an IC50 value of 1.1 μM. F44-A13 can optimize cholesterol metabolism and reduce its activity by inducing CYP7A1 expression. F44-A13 reduces levels of cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-C) in mouse models. F44-A13 can be used in the study of metabolic diseases associated with lipid disorders.
  • HY-120875
    HX600
    		Agonist 99.40%
    HX600 is a synthetic agonist for RXR (Retinoid X Receptor) heterodimer complex. HX600 prevents ischemia-induced neuronal damage. HX600 has orally bioactivity.
  • HY-N10361
    Drupanin
    		Agonist 99.35%
    Drupanin is an orally active and selective AKR1C3 enzyme inhibitor and an RXRα agonist with an EC50 value of 4.8 μM, which is found in green propolis. Drupanin also activates PPARγ moderately. Drupanin induces adipogenesis and elevates aP2 mRNA levels in 3T3-L1 fibroblasts Drupanin has the potential for the research of breast and prostate cancers.
  • HY-183986
    SR210831C
    		Inhibitor
    SR210831C is a highly selective, orally active retinoic acid receptor α (RARα) inhibitor with an IC50 of 0.051 nM. SR210831C suppresses spermatogenesis by reducing sperm count in house mice via acting on the early stages of spermatogenesis, and it does not cross the blood-testis barrier. SR210831C can be used in male contraception research.
  • HY-167262
    AGN-191659
    		Agonist
    AGN-191659 is an orally active RAR/RXR agonist with EC50 values of 11 nM, 23 nM, and 37 nM for RXRα, RARβ, and RARγ, respectively. AGN-191659 activates RXRα, RARβ and RARγ to induce gene transcription. AGN-191659 induces tissue transglutaminase activity, inhibits ornithine decarboxylase activity induced by tumor promoters, and suppresses chondrogenesis. AGN-191659 reverses basic fibroblast growth factor-induced endothelial cell proliferation. AGN-191659 induces hypertriglyceridemia in rat models. AGN-191659 inhibits total heparin-releasable lipase activity. AGN-191659 can be used in research related to promyelocytic leukemia and hypertriglyceridemia.
  • HY-119574
    GW0791
    		Agonist
    GW0791 (Compound 3) is an RXRα agonist with an EC50 of 5 nM. GW0791 can be used for cancer research.
  • HY-121435
    K-8012
    		Antagonist 99.51%
    K-8012 is a Sulindac (HY-B0008) analog and RXRα antagonist with an IC50 of 9.2 µM. K-8012 inhibits the activation of AKT. K-8012 induces Apoptosis, redirecting the TNFα signaling pathway from survival to death. K-8012 exerts anticancer activity against lung cancer, prostate cancer, and breast cancer. K-8012 can be used in research related to lung cancer, prostate cancer, breast cancer, and hepatocellular carcinoma.
  • HY-111844
    PROTAC RAR Degrader-1
    		Inhibitor
    PROTAC RAR degrader-1 (Compound 9) is a potent and selective RAR PROTAC Degrader consisting of apoptotic protein inhibitors (IAPs) ligands. IAPs-based degraders are also known as SNIPERs. PROTAC RAR Degrader-1 reduces RARα levels in HT1080 cells in a concentration-dependent manner but is blocked by the proteasome inhibitor MG132 (HY-13259). PROTAC RAR Degrader-1 can be used in the study of nuclear receptor-related diseases. (Pink: RAR ligand 1 (HY-111843); Black: Linker (HY-140189); Blue: IAPs Ligand (HY-B0134)).
  • HY-U00449A
    AGN 193109 sodium
    		Antagonist
    AGN 193109 sodium is the sodium salt form of AGN 193109 (HY-U00449). AGN 193109 sodium is the pan antagonist for retinoic acid receptor (RAR), with Kd of 2, 2 and 3 nM, for RARα, RARβ and RARγ, respectively. AGN 193109 sodium reverses TTNPB-induced morphology changes and all-trans retinoic acid (tRA)/9-cis RA/13-cis RA-induced proliferation suppression in ECE16-1 cell. AGN 193109 sodium is the antidote for retinoic acidosis, that ameliorates the skin and mucosal toxicity.
  • HY-180182
    RXR agonist 3
    		Agonist
    RXR agonist 3 (Compound 35) is a potent, partial RXR agonist (EC50s: 3, 3, 8 nM for RXRα, RXRβ, RXRγ, respectively). RXR agonist 3 can be used in the research of Alzheimer's disease, multiple sclerosis, and lymphoma.
  • HY-149085A
    (E)-XS-060
    		Antagonist
    (E)-XS-060 is an isomer of XS-060. XS-060 is a RXRα antagonist. XS-060 inhibits pRXRα-PLK1 interaction. XS-060 induces RXRα-dependent mitotic arrest. XS-060 exhibits good antitumor activity against breast cancer, lung adenocarcinoma, and liver cancer.
Cat. No. Product Name / Synonyms Application Reactivity