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

RAR/RXR

Retinoic acid receptors; Retinoid X receptors

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-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-14799
    Palovarotene
    Agonist 99.82%
    Palovarotene is a nuclear retinoic acid receptor γ (RAR-γ) agonist.
    Palovarotene
  • HY-107399
    CD3254
    Agonist 98.18%
    CD3254 a potent and selective retinoid-X-receptor (RXR) agonist.
    CD3254
  • HY-16681
    AGN 194310
    Antagonist 98.07%
    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-108527
    CD1530
    Agonist 98.13%
    CD1530 is an orally active, selective RARγ agonist and antibacterial agent. CD1530 reduces Smad1/5/8 phosphorylation and overall Smad levels. CD1530 reduces β-catenin, MMP9 protein, and ROS levels. CD1530 exhibits activities such as inhibiting heterotopic ossification, promoting Achilles tendon healing, and inhibiting muscle fatty infiltration. CD1530 can be used in the research of orthopedic diseases (such as heterotopic ossification, Achilles tendon injury), muscle diseases (such as muscle fatty infiltration-related diseases).
    CD1530
  • 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-100256
    Trifarotene
    Agonist 99.12%
    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-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-100608
    BMS453
    Modulator 99.13%
    BMS453 (BMS-189453), a synthetic retinoid, is a RARβ agonist and a RARα/RARγ antagonist. BMS453 inhibits breast cell growth predominantly through the induction of active TGFβ.
    BMS453
  • 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-107765
    LY2955303
    Antagonist 99.80%
    LY2955303 is a potent and selective retinoic acid receptor gamma (RARγ) antagonist with a Ki of 1.09 nM.
    LY2955303
  • 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-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-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-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-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-13717
    AGN194204
    Activator 99.94%
    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-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-W014589
    2,4-Di-tert-butylphenol
    Activator 99.99%
    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 -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
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