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-N0163R
    Magnolol (Standard)
    Agonist
    Magnolol (Standard) is the analytical standard of Magnolol. This product is intended for research and analytical applications. Magnolol, a natural lignan isolated from the stem bark of Magnolia officinalis, is a dual agonist of both RXRα and PPARγ, with EC50 values of 10.4 μM and 17.7 μM, respectively.
    Magnolol (Standard)
  • HY-118364
    AGN 190727
    AGN 190727 is a structural isomer of AGN 190121 and has no activating effect on RAR/RXR. AGN 190121 is a RAR-specific agonist that causes a dose-dependent increase in serum triglycerides, leading to hypertriglyceridemia.
    AGN 190727
  • HY-149085A
    (E)-XS-060
    Antagonist
    (E)-XS-060 is an isomer of XS-060. XS-060 is a RXRα antagonist. XS-060 inhibits pRXRα-PLK1 interaction. XS-060 induces RXRα-dependent mitotic arrest. XS-060 exhibits good antitumor activity against breast cancer, lung adenocarcinoma, and liver cancer.
    (E)-XS-060
  • HY-100532R
    CD437 (Standard)
    Agonist
    CD437 (Standard) is the analytical standard of CD437. This product is intended for research and analytical applications. CD437 is a selective Retinoic Acid Receptor γ (RARγ) agonist.
    CD437 (Standard)
  • HY-14171S2
    Bexarotene-13C6
    Agonist
    Bexarotene-13C6 (LGD1069-13C6) is 13C labeled Bexarotene. Bexarotene (LGD1069) is a high-affinity and selective retinoid X receptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM). Bexarotene can be used for the research of cutaneous T-cell lymphoma.
    Bexarotene-<sup>13</sup>C<sub>6</sub>
  • HY-B0091A
    Adapalene sodium salt
    Agonist
    Adapalene (CD271) sodium salt, a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene sodium salt is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene sodium salt also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene sodium salt exhibits anti-tumor activity.
    Adapalene sodium salt
  • HY-118420
    BMS-185411
    Antagonist
    BMS-185411 is a selective retinoic acid receptor alpha (RARα) antagonist, with an IC50 value of 140 nM.
    BMS-185411
  • HY-B0107A
    Acitretin sodium
    Agonist
    Acitretin (Ro 10-1670) sodium is a second-generation, systemic retinoid that has been used in the treatment of psoriasis. Acitretin sodium also can be used for the research of Alzheimer’s disease.
    Acitretin sodium
  • HY-16685
    AGN 205327
    Agonist
    AGN 205327 is a potent synthetic RARs agonist with EC50 of 3766/734/32 nM for RARα/β/γ respectively; no inhibition on RXR.
    AGN 205327
  • HY-106019CR
    Liarozole dihydrochloride (Standard)
    Inhibitor
    Liarozole (dihydrochloride) (Standard) is the analytical standard of Liarozole (dihydrochloride). This product is intended for research and analytical applications. Liarozole (R75251) dihydrochloride is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole dihydrochloride inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of RA (IC50=7 μM), resulting in increased tissue levels of RA. Liarozole dihydrochloride shows antitumoral properties[1][2][3].
    Liarozole dihydrochloride (Standard)
  • HY-14171R
    Bexarotene (Standard)
    Agonist
    Bexarotene (Standard) is the analytical standard of Bexarotene. This product is intended for research and analytical applications. Bexarotene (LGD1069) is a high-affinity and selective retinoid X receptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM). Bexarotene can be used for the research of cutaneous T-cell lymphoma.
    Bexarotene (Standard)
  • HY-106019R
    Liarozole (Standard)
    Inhibitor
    Liarozole (Standard) is the analytical standard of Liarozole. This product is intended for research and analytical applications. Liarozole (R75251; R85246) is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of retinoic acid (IC50=7 μM), resulting in increased tissue levels of retinoic acid. Liarozole shows antitumoral properties[1][2][3].
    Liarozole (Standard)
  • HY-15388S2
    Tazarotene-13C6
    Agonist
    Tazarotene-13C6 (AGN 190168-13C6) is 13C labeled Tazarotene. 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-<sup>13</sup>C<sub>6</sub>
  • HY-14649S6
    Retinoic acid-d3-1
    Agonist
    Retinoic acid-d3-1 is the deuterium labeled Retinoic acid (HY-14649). 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.
    Retinoic acid-d<sub>3</sub>-1
  • HY-15127S
    Isotretinoin-d5
    Agonist
    Isotretinoin-d5 is the deuterium labeled Isotretinoin. Isotretinoin is an orally active vitamin A derivative and is often be used for the research of severe acne. Isotretinoin also shows anticancer activity[1][2][3].
    Isotretinoin-d<sub>5</sub>
  • HY-107218
    11-Hydroxysugiol
    Modulator
    11-Hydroxysugiol regulates the SUMOylation of intracellular receptors by modulating RARα and vitamin D3 receptor (VDR).
    11-Hydroxysugiol
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