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

RAR/RXR

Retinoic acid receptors; Retinoid X receptors

RAR/RXR

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The nuclear retinoic acid receptors (RARs) are transcriptional transregulators, which control the expression of specific gene subsets subsequently to ligand binding and to strictly controlled phosphorylation processes. RARs consist of three subtypes, α (NR1B1), β (NR1B2) and γ (NR1B3), encoded by separate genes. RARs function as ligand-dependent transcriptional regulators, heterodimerized with retinoid X receptors (RXRs), which also consist of three types, α NR2B1, β (NR2B2) and γ (NR2B3). RARs play critical roles in a variety of biological processes, including development, reproduction, immunity, organogenesis and homeostasis, as assessed by vitamin A-deficiency (VAD), pharmacological and genetic studies conducted in the mouse.

Retinoid X receptor (RXR) belongs to a family of ligand-activated transcription factors that regulate many aspects of metazoan life. A class of nuclear receptors requires RXR as heterodimerization partner for their function.

RAR/RXR Isoform Specific Products:

RAR/RXR Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-107395
    BMS 753
    		Agonist ≥99.0%
    BMS 753 is an isotype-selective retinoic acid receptor α (RARα) agonist, with a Ki of 2 nM.
    BMS 753
  • 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.
    2,4-Di-tert-butylphenol
  • HY-16684
    AGN-195183
    		Agonist 99.75%
    AGN-195183 (IRX-5183) is a potent and selective agonist of RARα (Kd=3 nM) with improved binding selectivity relative to AGN 193836. AGN-195183 has no activity on RARβ/γ.
    AGN-195183
  • HY-106019
    Liarozole
    		Inhibitor 98.96%
    Liarozole (R75251; R85246) is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of retinoic acid (IC50=7 μM), resulting in increased tissue levels of retinoic acid. Liarozole shows antitumoral properties.
    Liarozole
  • HY-108523
    LG100754
    		Modulator 99.0%
    LG100754 (UVI 2112) is a RXR dimers modulater. LG100754 acts as a RXR:RXR homodimer antagonist, but functions as a agonist towards RXR:PPARα and RXR:PPARγ heterodimers. LG100754 is an insulin sensitizer that functions through RXR.
    LG100754
  • HY-101259
    BMS-195614
    		Antagonist 99.5%
    BMS-195614 (BMS 614) is an orally active neutral RARα-selective antagonist with a Ki of 2.5 nM. BMS-195614 restores the expression of Bcl2. BMS-195614 inhibits the transactivation of NF-κB, AP-1 and PPAR. BMS-195614 downregulates the expression of IL-6 and VEGF. BMS-195614 reduces blue light-induced phototoxicity and inhibits cell migration. BMS-195614 modulates inflammation and angiogenesis.
    BMS-195614
  • HY-107437
    CD2665
    		Antagonist 99.68%
    CD2665 is an orally active and selective RAR-β,γ antagonist, with Kd values of 306 nM, 110 nM for RAR-β and RAR-γ, repectively.
    CD2665
  • HY-108522
    PA452
    		Antagonist ≥99.0%
    PA452, retinoic X receptor (RXR) specific antagonist, inhibits the effect of Retinoic acid (RA) on Th1/Th2 development.
    PA452
  • HY-108533
    CD2314
    		Agonist 99.84%
    CD2314 is a potent and selective RARβ receptor agonist with a Kd of 195 nM in S91 melanoma cells.
    CD2314
  • HY-10291
    Tarenflurbil
    		Inhibitor 99.95%
    Tarenflurbil ((R)-Flurbiprofen) is the R-enantiomer of the racemate NSAID Flurbiprofen, Tarenflurbil ((R)-Flurbiprofen) inhibits the binding of [3H]9-cis-RA to RXRα LBD with IC50 of 75 μM. Tarenflurbil can be used for Alzheimer's disease research.
    Tarenflurbil
  • HY-14649S4
    Retinoic acid-d5
    		Agonist 99.07%
    Retinoic acid-d5 is the the deuterium labeled Retinoic acid (HY-14649). Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha.
    Retinoic acid-d<sub>5</sub>
  • 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.
    ER 50891
  • HY-16682
    AGN 196996
    		Antagonist 99.76%
    AGN 196996 is a potent and selective RARα antagonist with Ki value of 2 nM; little binding affinity for RARβ(Ki=1087 nM) and RARγ(Ki=8523 nM).
    AGN 196996
  • 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.
    F44-A13
  • HY-116506
    Bigelovin
    		Inhibitor 99.92%
    Bigelovin, a sesquiterpene lactone isolated from Inula hupehensis, is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation.
    Bigelovin
  • HY-111573
    KCL-286
    		Agonist 98.93%
    KCL-286 (C286) is an orally active and brain-penetrant retinoic acid receptor (RAR) β2 agonist (EC50 = 1.9 nM). KCL-286 targets RARβ2 with good selectivity over RAR α (EC50 = 26 nM) and RAR γ (EC50 = 11 nM). KCL-286 activates RARβ2 in the injured neurons. KCL-286 induces axonal regeneration of both spinal and sensory nerves through the inhibitory environment of the CNS, modulates neuroinflammation and extracellular matrix molecules. KCL-286 can modulate the expression of CSPGs by neuronal secretion of decorin which promotes myelination and aids axonal growth. KCL-286 can be studied in research for area such as spinal cord injury and traumatic nerve injury.
    KCL-286
  • HY-16683
    AGN 205728
    		Antagonist 98.62%
    AGN 205728 is a potent and selective RARγ antagonist with Ki/IC95 values of 3 nM/0.6 nM; no inhibiton on RARα and RARβ. AGN 205728 can inhibit abnormal proliferation of leukemia cells.
    AGN 205728
  • HY-119518
    BMS641
    		Agonist 98.12%
    BMS641 (BMS-209641) is a selective RARβ agonist. BMS641 has a higher affinity for RARβ (Kd, 2.5 nM) that is 100 times higher than that for RARα (Kd, 225 nM) or RARγ (Kd, 223 nM).
    BMS641
  • HY-B0877
    Halcinonide
    		Inhibitor 98.29%
    Halcinonide (SQ-18566) is an orally active Smoothened (Smo) agonist. Halcinonide activates the Hedgehog signaling pathway by binding to Smo and promoting its internalization and expression, thereby activating Gli transcription factors. Halcinonide not only stimulates cell proliferation, increases the expression of cyclin D2/CDK6 and inhibits the degradation of caspase-3, but also suppresses Bcl-2/Bax-mediated apoptosis, oxidative stress and inflammatory responses. Halcinonide activates RxRγ to upregulate the expression of myelin genes, thereby reducing cerebral infarction and improving behavioral deficits. Halcinonide has been used in studies related to multiple sclerosis and ischemic stroke.
    Halcinonide
  • HY-125904
    4-Hydroxyretinoic acid
    		Activator
    4-Hydroxyretinoic acid (4-HRA) is a derivative of Retinoic acid (HY-14649). 4-Hydroxyretinoic acid is formed via the catalysis of retinol by cytochrome P-450 isoenzymes. 4-Hydroxyretinoic acid also serves as a substrate for UDP-glucuronosyltransferase (s) and recombinant UGT2B7. 4-Hydroxyretinoic acid binds to the nuclear receptor RAR (Retinoic Acid Receptor), activates RAR and RXR-alpha, subsequently regulates gene expression and cell differentiation, and induces cancer cell apoptosis (Apoptosis). 4-Hydroxyretinoic acid also participates in multiple physiological processes such as immunoregulation, neuroprotection and antioxidation.
    4-Hydroxyretinoic acid
Cat. No. Product Name / Synonyms Application Reactivity
RAR/RXR Isoform Comparison

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