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

Related Products

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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-108530
    MM11253
    		Antagonist 98.21%
    MM11253 is a potent and selective RARγ antagonist with an IC50 of 44 nM. MM11253 has lower inhibition of RARα, RARβ and RXRα. MM11253 blocks the growth inhibitory effects of RARγ-selective agonists.
    MM11253
  • 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-153122A
    YCT529
    		Inhibitor ≥98.0%
    YCT529 is a potent, selective and orally active RAR-α inhibitor.
    YCT529
  • 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-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-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-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 99.91%
    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-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-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-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-101953
    β-Apo-13-carotenone
    		Antagonist
    β-Apo-13-carotenone (D'Orenone) is a naturally occurring β-apocarotenoid functioned as an antagonist of RXRα.
    β-Apo-13-carotenone
  • HY-106019
    Liarozole
    		Inhibitor 98.83%
    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-124136
    WYC-209
    		Agonist 99.82%
    WYC-209, a synthetic retinoid, is a retinoic acid receptor (RAR) agonist. WYC-209 induces apoptosis primarily via the caspase 3 pathway (IC50=0.19 μM for inmalignant murine melanoma TRCs), and has long-term effects with little toxicity.
    WYC-209
  • 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-144377
    RXR antagonist 1
    		Modulator 99.94%
    RXR antagonist 1 (compound 6a) is a retinoid X receptor (RXR) modulator. RXR antagonist 1 shows potent RXR-antagonistic activity, with a pA2 of 8.06. RXR antagonist 1 can be used for type 2 diabetes research.
    RXR antagonist 1
  • HY-125904
    4-Hydroxyretinoic acid
    		Activator
    4-Hydroxyretinoic acid (4-HRA) is a naturally occurring retinoid derivative with diverse biological effects. 4-Hydroxyretinoic acid is formed from retinol catalyzed by cytochrome P-450 isozyme(s), and is mainly metabolized by the liver in the body. 4-Hydroxyretinoic acid also serves as the substrate for human liver microsomal UDP-glucuronosyltransferase(s) and recombinant UGT2B7. 4-Hydroxyretinoic acid regulates gene expression and cell differentiation via binding to nuclear receptor RAR (Retinoic Acid Receptor), and activates RARs and RXR-alpha, to induce cancer cell apoptosis. In addition, 4-Hydroxyretinoic acid is also involved in various physiological processes such as immune regulation, neuroprotection, and anti-oxidation.
    4-Hydroxyretinoic acid
  • HY-14649S4
    Retinoic acid-d5
    		Agonist 98.25%
    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-16683
    AGN 205728
    		Antagonist 98.62%
    AGN 205728 is a potent and selective RARγ antagonist with Ki/IC95 values of 3 nM/ 0.
    AGN 205728
Cat. No. Product Name / Synonyms Application Reactivity
RAR/RXR Isoform Comparison

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