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 (85):

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 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.
  • HY-15682
    TTNPB
    Agonist 98.81%
    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-10475
    AM580
    Agonist 99.61%
    AM580 is a selective RARα agonist with IC50 and EC50 of 8 nM and 0.36 nM, respectively.
  • HY-101106
    AR7
    Antagonist 98.85%
    AR7 is an atypical RARA/RARα (retinoic acid receptor, alpha) antagonist. AR7 specifically activates chaperone-mediated-autophagy (CMA) activity without affecting macroautophagy.
  • HY-108521
    HX531
    Antagonist 99.22%
    HX531 is a potent RXR antagonist with an IC50 of 18 nM. It has been shown to reduce triglyceride content in white adipose tissue, skeletal muscle, and the liver of mice on a high fat diet.
  • HY-108527
    CD1530
    Agonist ≥98.0%
    CD1530 is a selective RARγ agonist with an Kd of 150 nM. CD1530 has been used in combination with bexarotene to inhibit oral carcinogenesis induced by the carcinogen 4-nitroquinoline 1-oxide in a mouse model of human oral-cavity and esophageal squamous-cell carcinoma.
  • HY-108533
    CD2314
    Agonist ≥99.0%
    CD2314 is a potent and selective RARβ receptor agonist with a Kd of 195 nM in S91 melanoma cells.
  • HY-U00449
    AGN 193109
    Antagonist 99.31%
    AGN 193109 is a retinoid analog, and acts as a specific and highly effective antagonist of retinoic acid receptors (RARs), with Kds of 2 nM, 2 nM, and 3 nM for RARα, RARβ, and RARγ, respectively.
  • HY-108529
    BMS493
    Inhibitor 98.46%
    BMS493 is an inverse pan-retinoic acid receptor (RAR) agonist. BMS493 increases nuclear corepressor interaction with RARs. BMS493 also could prevent retinoic acid-induced differentiation.
  • HY-15127
    Isotretinoin
    Inhibitor 99.53%
    Isotretinoin(13-cis-Retinoic acid) is a medication used for the treatment of severe acne.
  • HY-100532
    CD437
    Agonist ≥98.0%
    CD437 is a selective Retinoic Acid Receptor γ (RARγ) agonist.
  • 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-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-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-107500
    UVI 3003
    Inhibitor 99.77%
    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-B0091
    Adapalene
    Agonist ≥98.0%
    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.
  • HY-16681
    AGN 194310
    Antagonist 98.01%
    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-N0163
    Magnolol
    Agonist 99.92%
    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.
Isoform Specific Products

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