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-W014589R
    2,4-Di-tert-butylphenol (Standard)
    Activator
    2,4-Di-tert-butylphenol (Standard) is the analytical standard of 2,4-Di-tert-butylphenol (HY-W014589). This product is intended for research and analytical applications. 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 pharmaceuticals and fragrances.
    2,4-Di-tert-butylphenol (Standard)
  • HY-120875
    HX600
    Agonist 99.40%
    HX600 is a synthetic agonist for RXR (Retinoid X Receptor) heterodimer complex. HX600 prevents ischemia-induced neuronal damage. HX600 has orally bioactivity.
    HX600
  • 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-100273
    AGN 194078
    Agonist 99.87%
    AGN 194078 is a selective RARα agonist with a Kd and EC50 of 3 and 112 nM, respectively.
    AGN 194078
  • HY-N10361
    Drupanin
    Agonist 99.35%
    Drupanin is an orally active and selective AKR1C3 enzyme inhibitor and an RXRα agonist with an EC50 value of 4.8 μM, which is found in green propolis. Drupanin also activates PPARγ moderately. Drupanin induces adipogenesis and elevates aP2 mRNA levels in 3T3-L1 fibroblasts Drupanin has the potential for the research of breast and prostate cancers.
    Drupanin
  • HY-108532
    AC-261066
    Agonist 99.27%
    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-108528
    BMS961
    Agonist 98.06%
    BMS961 is a selective retinoic acid receptor-γ (RARγ) agonist. BMS961 shows anti-inflammatory activity.
    BMS961
  • 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-14802C
    (+)-Talarozole
    Inhibitor 99.78%
    (+)-Talarozole is a potent inhibitor of retinoic acid metabolism extracted from patent WO 1997049704 A1.
    (+)-Talarozole
  • HY-149085
    XS-060
    Antagonist 98.67%
    XS-060 is a potent anticancer agent and RXRα antagonist. XS-060 significantly induces RXRα-dependent mitotic arrest by inhibiting pRXRα-PLK1 interaction. XS-060 inhibits p-RXRα interaction with PLK1 but has no effect on RXRα heterodimerization with RARγ. XS-060 inhibits the in situ interaction between p-RXRα and PLK1 at the centrosome.
    XS-060
  • HY-14653
    Amsilarotene
    Inhibitor 99.67%
    Amsilarotene (TAC-101; Am 555S), an orally active synthetic retinoid, has selective affinity for retinoic acid receptor α (RAR-α) binding with Ki of 2.4, 400 nM for RAR-α and RAR-β. Amsilarotene induces the apoptotic of human gastric cancer, hepatocellular carcinoma and ovarian carcinoma cells. Amsilarotene can be used for the research of cancer.
    Amsilarotene
  • HY-108526
    AC-55649
    Agonist 99.70%
    AC-55649 is a potent, highly isoform-selective agonist of human RARβ2 receptor, with a pEC50 of 6.9.
    AC-55649
  • HY-108531A
    ER 50891 quarterhydrate
    Antagonist 99.86%
    ER 50891 quarterhydrate 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 quarterhydrate
  • HY-153832
    MSU-42011
    Agonist 99.64%
    MSU-42011 is an orally active retinoid X receptor (RXR) agonist. MSU-42011 inhibits the iNOS activity and reduces the expression of p-ERK protein. MSU-42011 has immunomodulatory and antitumor activity.
    MSU-42011
  • HY-121435
    K-8012
    Antagonist 99.51%
    K-8012 is a Sulindac (HY-B0008) analog and RXRα antagonist with an IC50 of 9.2 µM. K-8012 inhibits the activation of AKT. K-8012 induces Apoptosis, redirecting the TNFα signaling pathway from survival to death. K-8012 exerts anticancer activity against lung cancer, prostate cancer, and breast cancer. K-8012 can be used in research related to lung cancer, prostate cancer, breast cancer, and hepatocellular carcinoma.
    K-8012
  • HY-132334S
    9-cis-Retinoic acid-d5
    Agonist 99.24%
    9-cis-Retinoic acid-d5 is the deuterium labeled 9-cis-Retinoic acid. 9-cis-Retinoic acid (ALRT1057), a vitamin A derivative, is a potent RAR/RXR agonist. 9-cis-Retinoic acid induces apoptosis, regulates cell cycle and has anticancer, anti-inflammatory and neuroprotection activities.
    9-cis-Retinoic acid-d<sub>5</sub>
  • HY-105689
    AGN 192870
    Antagonist 98.49%
    AGN 192870 is a RAR neutral antagonist with Kds of 147, 33, and 42 nM for RARα, RARβ, and RARγ, respectively. AGN 192870 shows IC50s of 87 and 32 nM for RARαand RARγ, respectively. AGN 192870 shows RARβ partial agonism. AGN 192870 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 192870
  • HY-114071
    BMS270394
    Agonist 98.0%
    BMS270394 is a nuclear retinoic acid receptor (RAR-γ) agonist with the EC50 values of 30 nM and 400 nM for humanRAR-γ and RAR-β, respectively.
    BMS270394
  • HY-A0067S
    Oxybenzone-d5
    99%
    Oxybenzone-d5 is the deuterium labeled Oxybenzone. 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-d<sub>5</sub>
  • HY-156280
    RARα antagonist 1
    Antagonist 99.07%
    RARα antagonist 1 (compound 21) is an orally active and selective retinoic acid receptor α(RARα) antagonist, with the IC50 of 4.6nM.
    RARα antagonist 1
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