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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-107436
    LE135
    		Antagonist 99.03%
    LE135 is a potent RAR antagonist that binds selectively to RARα (Ki of 1.4 μM) and RARβ (Ki of 220 nM), and has a higher affinity to RARβ. LE135 is highly selective over RARγ, RXRα, RXRβ and RXRγ. LE135 is also a potent TRPV1 and TRPA1 receptors activator with EC50s of 2.5 μM and 20 μM, respectively.
    LE135
  • HY-153122A
    YCT529
    		Inhibitor ≥98.0%
    YCT529 is a potent, selective and orally active RAR-α inhibitor.
    YCT529
  • HY-111844
    PROTAC RAR Degrader-1
    		Inhibitor
    PROTAC RAR Degrader-1 comprises a IAP ligand binding group, a linker and a RAR ligand binding group. PROTAC RAR Degrader-1 is an RAR degrader. Maximal RAR degradation at 30 μM concentration in HT1080 cells. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs).
    PROTAC RAR Degrader-1
  • 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-108532
    AC-261066
    		Agonist 98.79%
    AC-261066 is a potent, orally available and isoform-selective retinoic acid beta2 (RARbeta2) receptor agonist, with a pEC50 of 8.0.
    AC-261066
  • HY-104070
    LG-100064
    		Agonist 99.66%
    LG-100064 is a retinoid-X-receptor (RXR) agonist, with EC50s of 330 nM, 200 nM, and 260 nM for RXRα, RXRβ and RXRγ; LG-100064 can be used in the research of cancer.
    LG-100064
  • HY-108530
    MM11253
    		Antagonist 98.64%
    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-107395
    BMS 753
    		Agonist 99.46%
    BMS 753 is an isotype-selective retinoic acid receptor α (RARα) agonist, with a Ki of 2 nM.
    BMS 753
  • 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-124136
    WYC-209
    		Agonist 98.68%
    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-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-101259
    BMS-195614
    		Antagonist 99.06%
    BMS-195614 (BMS 614) is a neutral RARα-selective antagonist with a Ki of 2.5 nM.
    BMS-195614
  • 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-108526
    AC-55649
    		Agonist 99.66%
    AC-55649 is a potent, highly isoform-selective agonist of human RARβ2 receptor, with a pEC50 of 6.9.
    AC-55649
  • 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-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-16682
    AGN 196996
    		Antagonist 99.87%
    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-119518
    BMS641
    		Agonist 98.24%
    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-106019C
    Liarozole dihydrochloride
    		Inhibitor ≥99.0%
    Liarozole (R75251) dihydrochloride is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole dihydrochloride inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of RA (IC50=7 μM), resulting in increased tissue levels of RA. Liarozole dihydrochloride shows antitumoral properties.
    Liarozole dihydrochloride
Cat. No. Product Name / Synonyms Application Reactivity