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-D1190
    DC271
    Agonist
    DC271 is a RAR agonist that can be considered a retinoid, eliciting cellular responses consistent with the endogenous retinoid ATRA and the synthetic retinoid EC23. DC271 binds to retinoid protein machinery, including CRABPII, to translocate the endogenous retinoid ATRA into the nucleus.
    DC271
  • HY-170863
    ZSH-2208
    Agonist 99.90%
    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-106735
    Arotinoid
    Agonist 99.55%
    Arotinoid (RO 13-6298) is a retinoid, and acts as an orally active and highly potent agonist of retinoic acid receptors (RARs) with antipsoriatic effects. Arotinoid has antipapiltoma activity with an ED50 of 0.05 mg/kg. Arotinoid can be used for the research of skin carcinomas.
    Arotinoid
  • HY-108525
    Fluorobexarotene
    Agonist 99.48%
    Fluorobexarotene (compound 20) is a potent retinoid-X-receptor (RXR) agonist, with a Ki value of 12 nM and an EC50 value of 43 nM for RXRα receptor. Fluorobexarotene possesses an apparent RXR binding affinity that is 75% greater than Bexarotene.
    Fluorobexarotene
  • HY-14171S
    Bexarotene-d4
    Agonist 98.51%
    Bexarotene-d4 is a deuterium labeled Bexarotene (LGD1069). Bexarotene (LGD1069) is a selective retinoid X receptors (RXR) agonist for the treatment of cutaneous T-cell lymphoma.
    Bexarotene-d<sub>4</sub>
  • HY-14649S3
    Retinoic acid-d6
    98.9%
    Retinoic acid-d6 is the deuterium labeled Retinoic acid[1]. Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha[2][3][4][5][6][7].
    Retinoic acid-d<sub>6</sub>
  • HY-10475G
    AM580 (GMP)
    Agonist
    AM580 (CD336) (GMP) is AM580= (HY-10475) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. AM580 is a selective RARα agonist.
    AM580 (GMP)
  • HY-112077A
    Viaminate
    Activator
    Viaminate is a derivative of Retinoic acid, which is used for the treatment of severe acne and other keratinization disorders.
    Viaminate
  • 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-141793
    ATRA-biotin
    Agonist 98.43%
    ATRA-biotin (Biotin-ATRA-conjugate) is a biotin-conjugated ATRA. ATRA-biotin can be used to track ATRA in cells or a given tissue.
    ATRA-biotin
  • HY-153165
    RXR antagonist 5
    Inhibitor 98.80%
    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-N2992
    16α-Hydroxytrametenolic acid
    Activator 98.0%
    16α-Hydroxytrametenolic acid, a natural triterpene, is a potential retinoid X receptor (RXR) selective agonist.
    16α-Hydroxytrametenolic acid
  • HY-14802D
    (-)-Talarozole
    Inhibitor 98.12%
    (-)-Talarozole is a potent inhibitor of retinoic acid metabolism extracted from patent WO 1997049704 A1.
    (-)-Talarozole
  • HY-15388R
    Tazarotene (Standard)
    Agonist
    Tazarotene (Standard) is the analytical standard of Tazarotene. This product is intended for research and analytical applications. 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 (Standard)
  • HY-121435
    K-8012
    Antagonist 98.24%
    K-8012, a sulindac (HY-B0008) analog, is a potent antagonist of RXRa. The IC50 value for K-8012 to inhibit 9-cis-RA-induced Gal4-RXRa-LBD trans-activation were about 9.2 μM. K-8012 exerts improved anticancer activity over sulindac in a RXRa-dependent manner. K-8012 exhibits activity in inhibiting the tRXRa-mediated PI3K/AKT signaling pathway. K-8012 induces apoptosis and inhibits AKT activation by preventing tRXRa from binding to p85a.
    K-8012
  • HY-100008R
    Peretinoin (Standard)
    Inhibitor
    Peretinoin (Standard) is the analytical standard of Peretinoin. This product is intended for research and analytical applications. 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[1]. 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[2]. Peretinoin inhibits HCV RNA amplification and virus release by altering lipid metabolism with a EC50 of 9 μM[3].
    Peretinoin (Standard)
  • HY-133739
    NBD-125
    Inhibitor
    NBD-125 (B-12), a berberine analogue, is an RXRα activator, with an IC50 of 31.10 μM in KM12C cell.
    NBD-125
  • HY-U00449G
    AGN 193109 (GMP)
    Antagonist
    AGN 193109 (GMP) is AGN 193109 (HY-U00449) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. AGN 193109 is a specific and highly effective retinoic acid receptor (RAR) antagonist. AGN 193109 (GMP) 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 193109 is the antidote for retinoic acidosis, that ameliorates the skin and mucosal toxicity.
    AGN 193109 (GMP)
  • HY-149086
    BPA-B9
    Antagonist
    BPA-B9 is a RXRα ligand and antagonist targeting the pRXRα-PLK1 interaction. BPA-B9 has excellent RXRα-binding affinity (KD=39.29 ± 1.12 nM). BPA-B9 inhibits the proliferation of cancer cells by inducing mitotic arrest and cell apoptosis.
    BPA-B9
  • HY-14802C
    (+)-Talarozole
    Inhibitor 99.28%
    (+)-Talarozole is a potent inhibitor of retinoic acid metabolism extracted from patent WO 1997049704 A1.
    (+)-Talarozole
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