1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. RAR/RXR

RAR/RXR

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.

RAR/RXR Related Products (44):

Cat. No. Product Name Effect Purity
  • HY-14649
    Retinoic acid Agonist 99.74%
    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.
  • HY-14171
    Bexarotene Agonist 99.90%
    Bexarotene (LGD1069) is a selective retinoid X receptors (RXR) agonist for the treatment of cutaneous T-cell lymphoma.
  • HY-14531
    Talarozole Inhibitor 99.78%
    Talarozole (R115866) is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA) which increases intracellular levels of endogenous all-trans retinoic acid (RA). Talarozole inhibits both CYP26A1 and CYP26B1 with IC50s of 5.4 and 0.46 nM, respectively.
  • HY-10475
    AM580 Agonist 99.61%
    AM580 is a selective RARα agonist with IC50 and EC50 of 8 nM and 0.36 nM, respectively.
  • HY-15373
    Fenretinide Inhibitor 99.08%
    Fenretinide (4-HPR) is a synthetic retinoid deriverative, binding to the retinoic acid receptors (RAR) at concentrations necessary to induce cell death.
  • HY-15340
    LG100268 99.22%
    LG100268 (LG268) is a potent, selective and orally active retinoid X receptor (RXR) agonist with EC50 values of 4 nM, 3 nM, and 4 nM for RXR-α, RXR-β, and RXR-γ, respectively. LG100268 displays >1000-fold selectivity for RXR over RAR, the Ki values are 3.4 nM, 6.2 nM and 9.2 nM for RXR-α, RXR-β, and RXR-γ, respectively. LG100268 activates RXR homodimers to induce transcriptional activation. LG100268 can be used for the study of lung carcinogenesisy.
  • HY-15128
    9-cis-Retinoic acid Agonist
    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.
  • HY-116506
    Bigelovin Inhibitor
    Bigelovin, a sesquiterpene lactone isolated from Inula helianthus-aquatica, is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation.
  • HY-100532
    CD437 Agonist >98.0%
    CD437 is a selective Retinoic Acid Receptor γ (RARγ) agonist.
  • HY-N0163
    Magnolol Agonist 99.72%
    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.
  • HY-14652
    Tamibarotene Agonist 99.94%
    Tamibarotene is a retinoic acid receptor α/β (RARα/β) agonist, showing high selectivity over RARγ.
  • HY-15682
    TTNPB Agonist 99.19%
    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.
  • HY-107500
    UVI 3003 Inhibitor 99.03%
    UVI 3003 is a highly selective antagonist of retinoid X receptor (RXR), and inhibits xenopus and human RXRα in Cos7 cells, with IC50s of 0.22 and 0.24 μM, respectively.
  • HY-15127
    Isotretinoin Inhibitor 99.88%
    Isotretinoin(13-cis-Retinoic acid) is a medication used for the treatment of severe acne.
  • HY-16681
    AGN 194310 Antagonist >98.0%
    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.
  • HY-100008
    Peretinoin Inhibitor 99.79%
    Peretinoin is an oral acyclic retinoid 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.
  • HY-14799
    Palovarotene Agonist 99.77%
    Palovarotene is a nuclear retinoic acid receptor γ (RAR-γ) agonist.
  • HY-B0091
    Adapalene Agonist >98.0%
    Adapalene(CD-271; Differin), a synthetic retinoid, is a retinoic acid receptor agonist (RAR).
  • HY-16684
    AGN 195183 Agonist 98.40%
    AGN 195183 is a potent and selective agonist of RARα(Kd=3 nM) with improved binding selectivity relative to AGN 193836; no activity on RARβ/γ.
  • HY-15388
    Tazarotene Agonist 99.93%
    Tazarotene (AGN 190168) is a selective retinoic acid receptor (RAR) agonist for the treatment of plaque psoriasis and acne vulgaris.
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