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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-16681
    AGN 194310
    		Antagonist 98.01%
    AGN 194310 (VTP-194310) is a high affinity, potent and selective retinioic acid receptors (RARs) pan-antagonist with Kd values of 3 nM, 2 nM, 5 nM for RARα, RARβ, RARγ, respectively. AGN 194310 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    AGN 194310
  • HY-107399
    CD3254
    		Agonist 98.71%
    CD3254 a potent and selective retinoid-X-receptor (RXR) agonist.
    CD3254
  • HY-108521
    HX531
    		Antagonist 99.87%
    HX531 is a potent RXR antagonist with an IC50 of 18 nM. It has been shown to reduce triglyceride content in white adipose tissue, skeletal muscle, and the liver of mice on a high fat diet.
    HX531
  • HY-108527
    CD1530
    		Agonist 98.13%
    CD1530 is a selective RARγ agonist with an Kd of 150 nM. CD1530 has been used in combination with bexarotene to inhibit oral carcinogenesis induced by the carcinogen 4-nitroquinoline 1-oxide in a mouse model of human oral-cavity and esophageal squamous-cell carcinoma.
    CD1530
  • HY-107397
    Ch55
    		Agonist 99.86%
    Ch55 is a potent synthetic retinoid. Ch55 binds to RAR-α and RAR-β receptors with high affinity. Ch55 displays low affinity for cellular retinoic acid binding protein (CRABP). Ch55 is a potent inducer of the differentiation of HL60 cells with an EC50 of 200 nM. Ch55 can be used for cancer research.
    Ch55
  • HY-14799
    Palovarotene
    		Agonist 99.82%
    Palovarotene is a nuclear retinoic acid receptor γ (RAR-γ) agonist.
    Palovarotene
  • HY-100256
    Trifarotene
    		Agonist 98.96%
    Trifarotene (CD5789) is a potent and selective RARγ agonist. Trifarotene (CD5789) shows ∼65-fold and ∼16-fold selectivitiy for the RARγ (EC50=7.7 nM) over RARα (EC50=500 nM) and RARβ (EC50=125 nM), respectively.
    Trifarotene
  • HY-15388
    Tazarotene
    		Agonist 99.83%
    Tazarotene (AGN 190168) is a selective retinoic acid receptor (RAR) agonist for the treatment of plaque psoriasis and acne vulgaris. Tazarotene is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Tazarotene
  • HY-100008
    Peretinoin
    		Inhibitor 99.79%
    Peretinoin is an oral acyclic retinoid with a vitamin A-like structure that targets retinoid nuclear receptors such as retinoid X receptor (RXR) and retinoic acid receptor (RAR). Peretinoin reduces the mRNA level of sphingosine kinase 1 (SPHK1) in vitro by downregulating a transcription factor, Sp1. Peretinoin prevents the progression of non-alcoholic steatohepatitis (NASH) and the development of hepatocellular carcinoma (HCC) through activating the autophagy pathway by increased Atg16L1 expression. Peretinoin inhibits HCV RNA amplification and virus release by altering lipid metabolism with a EC50 of 9 μM.
    Peretinoin
  • HY-13717
    AGN194204
    		Activator ≥99.0%
    AGN194204 (IRX4204) is an orally active and selective RXR agonist with Kd values 0.4 nM, 3.6 nM and 3.8 nM and EC50s of 0.2 nM, 0.8 nM and 0.08 nM for RXRα, RXRβ and RXRγ, respectively. AGN194204 is inactive against RAR. AGN194204 has anti-inflammatory and anticarcinogenic actions.
    AGN194204
  • HY-16684
    AGN-195183
    		Agonist 99.76%
    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-107765
    LY2955303
    		Antagonist 98.60%
    LY2955303 is a potent and selective retinoic acid receptor gamma (RARγ) antagonist with a Ki of 1.09 nM.
    LY2955303
  • HY-A0067
    Oxybenzone
    		Modulator 99.94%
    Oxybenzone (Benzophenone 3) is a commonly used UV filter in sun tans and skin protectants. Oxybenzone act as endocrine disrupting chemicals (EDCs) and can pass through the placental and blood-brain barriers. Benzophenone-3 impairs autophagy, alters epigenetic status, and disrupts retinoid X receptor signaling in apoptotic neuronal cells.
    Oxybenzone
  • 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-116248
    Ro 41-5253
    		Antagonist 98.44%
    Ro 41-5253 is an orally active selective retinoic acid receptor alpha (RARα) antagonist. Ro 41-5253 can bind RARα without inducing transcription or affecting RAR/RXR heterodimerization and DNA binding. Ro 41-5253 can inhibit cancer cell proliferation and induce apoptosis, has antitumor activity.
    Ro 41-5253
  • HY-107413
    SR11237
    		Agonist 99.91%
    SR11237 (BMS-649) is a potent retinoid X receptor (RXR)-selective agonist that is devoid of any RAR activity. SR11237 can cause RXR/RXR homodimers to form and transactivate a reporter gene containing a RXR-response element.
    SR11237
  • 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-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-B0107
    Acitretin
    		Agonist 99.66%
    Acitretin (Ro 10-1670) is a second-generation, systemic retinoid that has been used in the treatment of psoriasis. Acitretin also can be used for the research of Alzheimer’s disease.
    Acitretin
  • HY-10291
    Tarenflurbil
    		Inhibitor 99.96%
    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
Cat. No. Product Name / Synonyms Application Reactivity