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-168885
    ZSH-512
    Inhibitor
    ZSH-512 is a potent RARγ inhibitor. ZSH-512 shows antiproliferation activity. ZSH-512 induces apoptosis. ZSH-512 decreases CD133, NANOG, SOX2, and EPCAM protein expression. ZSH-512 shows anticancer activity. ZSH-512 has the potential for the research of colorectal cancer.
    ZSH-512
  • HY-144383
    RXR antagonist 2
    Antagonist
    RXR antagonist 2 (compound 6b) is a potent antagonist of RXR with a Ki and Kd of 0.391 and 0.281 μM. RXR antagonist 2 has the potential for the research of RXR related diseases.
    RXR antagonist 2
  • HY-153165
    RXR antagonist 5
    Inhibitor
    RXR antagonist 5 (compound 22) is a selective retinoic acid X receptor (RXR) antagonist with binding potential to RXR evaluated by modeling.
    RXR antagonist 5
  • HY-10475R
    AM580 (Standard)
    Agonist
    AM580 (Standard) is the analytical standard of AM580. This product is intended for research and analytical applications. AM580 is a selective RARα agonist with IC50 and EC50 of 8 nM and 0.36 nM, respectively.
    AM580 (Standard)
  • HY-155437
    NEt-iFQ
    Agonist
    NEt-iFQ is a fluorescent retinoid X receptor (RXR) agonist with potent solvatochromic properties. NEt-iFQ selectively binds to RXR-LBP and fluoresces.
    NEt-iFQ
  • HY-U00449A
    AGN 193109 sodium
    Antagonist
    AGN 193109 sodium is the sodium salt form of AGN 193109 (HY-U00449). AGN 193109 sodium is the pan antagonist for retinoic acid receptor (RAR), with Kd of 2, 2 and 3 nM, for RARα, RARβ and RARγ, respectively. AGN 193109 sodium reverses TTNPB-induced morphology changes and all-trans retinoic acid (tRA)/9-cis RA/13-cis RA-induced proliferation suppression in ECE16-1 cell. AGN 193109 sodium is the antidote for retinoic acidosis, that ameliorates the skin and mucosal toxicity.
    AGN 193109 sodium
  • HY-A0067S
    Oxybenzone-d5
    Oxybenzone-d5 is the deuterium labeled Oxybenzone[1]. 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[2][3][4].
    Oxybenzone-d<sub>5</sub>
  • HY-138967
    BRF110
    BRF110 is the selective, orally active rexinoid for Nurr1-RXRα, that selectively activates the Nurr1-RXRα heterodimer with an EC50 of 0.9 μM in SH-SY5Y. BRF110 upregulates the expression of BDNF, exhibits neuroprotective activity against MPP+ induced toxicity. BRF110 can cross blood-brain barrier.
    BRF110
  • 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
  • HY-162162
    RXR agonist 1
    Agonist
    RXR agonist 1 (Compound 33) is a highly selective RXR agonist, with EC50s of 9 nM, 18 nM, and 11 nM for RXRα, RXRβ, and RXRγ, respectively. RXR agonist 1 binds to RXR with high affinity (Kd = 0.03 μM).
    RXR agonist 1
  • HY-108524
    LG101506
    Modulator
    LG101506 is a selective and orally active RXR modulator with a Ki of 2.7 nM for RXRα. LG101506 can be used for the research of type 2 diabetes and cancer.
    LG101506
  • HY-153980
    K-80001
    K-80001 is an RXRα-binder and COX-1/2 inhibitor, with IC50s of with an IC50 of 82.9μM, 3.4μM, 1.2μM for RXRα, COX-1 and COX-2, respectively.
    K-80001
  • HY-B0107R
    Acitretin (Standard)
    Agonist
    Acitretin (Standard) is the analytical standard of Acitretin. This product is intended for research and analytical applications. 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 (Standard)
  • HY-B0091S
    Adapalene-d3
    Agonist
    Adapalene-d3 is the deuterium labeled Adapalene. Adapalene (CD271), a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene exhibits anti-tumor activity[1][2][3].
    Adapalene-d<sub>3</sub>
  • HY-15682R
    TTNPB (Standard)
    Agonist
    TTNPB (Standard) is the analytical standard of TTNPB. This product is intended for research and analytical applications. TTNPB is a highly potent RAR agonist. Competitive binding assays using human RARs yield IC50s of α=5.1 nM, β= 4.5 nM, and γ=9.3 nM, respectively.
    TTNPB (Standard)
  • HY-117182
    LG190178
    LG190178 is a non-steroidal vitamin D receptor (VDR) ligand that can induce the formation of heterodimer complexes between VDR and retinoid X receptor (RXR), stabilizing the agonistic conformation of the VDR ligand-binding domain and promoting its interaction with co-activators. LG190178 has functions in regulating calcium homeostasis, bone mineralization, as well as cell proliferation, differentiation, and apoptosis, making it useful for research in psoriasis, osteoporosis, and cancer.
    LG190178
  • HY-170863
    ZSH-2208
    Agonist
    ZSH-2208 is an analog of retinoic acid A, which exerts a potent antitumor effect on regenerative stem cells (TRCs) of esophageal squamous cell carcinoma (ESCC) through RARγ-TNFAIP3.
    ZSH-2208
  • HY-170786
    IRX5010
    Agonist
    IRX5010 (IRX4647F), an analogue of IRX4647, is a highly selective RARγ nuclear receptor agonist. IRX5010 demonstrates inhibition of in vivo growth of EMT-6 triple negative breast cancer.
    IRX5010
  • HY-118761
    5,6-Epoxyretinoic acid
    Agonist
    all-trans-5,6-epoxy Retinoic acid (5,6-epoxy RA) is an agonist of all isoforms of the retinoic acid receptor (RAR; EC50s=77, 35, and 4 nM for RARα, RARβ, and RARγ, respectively). 5,6-epoxy RA (1 μM) also induces growth arrest of MCF-7 and NB4 cells in vitro. It is a natural metabolite of all-trans retinoic acid, which is a metabolite of vitamin A.
    5,6-Epoxyretinoic acid
  • HY-121671
    TBTC
    Activator
    TBTC is a selective agonist with the activity of improving behavioral deficits in Alzheimer's disease model mice. TBTC can effectively activate the heterodimerization of RXRα with LXRα or PPARγ. TBTC stimulates the expression of apoE, ABCA1, and ABCG1 genes and reduces Aβ content in cells and animal models.
    TBTC
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