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Inhibitors & Agonists




Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-107436
    1 Publications Verification

    RAR/RXR TRP Channel Neurological Disease Cancer
    LE135 is a potent RAR antagonist that binds selectively to RARα (Ki of 1.4 μM) and RARβ (Ki of 220 nM), and has a higher affinity to RARβ. LE135 is highly selective over RARγ, RXRα, RXRβ and RXRγ. LE135 is also a potent TRPV1 and TRPA1 receptors activator with EC50s of 2.5 μM and 20 μM, respectively .
  • HY-107413


    RAR/RXR Cancer
    SR11237 (BMS-649) is a potent retinoid X receptor (RXR)-selective agonist that is devoid of any RAR activity. SR11237 can cause RXR/RXR homodimers to form and transactivate a reporter gene containing a RXR-response element .
  • HY-108530

    RAR/RXR Cancer
    MM11253 is a potent and selective RARγ antagonist with an IC50 of 44 nM. MM11253 has lower inhibition of RARα, RARβ and RXRα. MM11253 blocks the growth inhibitory effects of RARγ-selective agonists .
  • HY-15340
    2 Publications Verification


    RAR/RXR Autophagy Metabolic Disease
    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-16685

    RAR/RXR Autophagy Cancer
    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-13717

    IRX4204; NRX194204; VTP 194204

    RAR/RXR Apoptosis Inflammation/Immunology Cancer
    AGN194204 (IRX4204) is an orally active and selective RXR agonist with Kd values 0.4 nM, 3.6 nM and 3.8 nM and EC50s of 0.2 nM, 0.8 nM and 0.08 nM for RXRα, RXRβ and RXRγ, respectively. AGN194204 is inactive against RAR. AGN194204 has anti-inflammatory and anticarcinogenic actions .
  • HY-14171
    Maximum Cited Publications
    16 Publications Verification


    RAR/RXR Autophagy Cancer
    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-111573

    RAR/RXR Others
    Anticancer agent 168 is an orally active retinoic acid receptor (RAR/RXR) beta2 agonist with ameliorating effects on spinal cord injury (SCI) .
  • HY-116248

    RAR/RXR Apoptosis Cancer
    Ro 41-5253 is an orally active selective retinoic acid receptor alpha (RARα) antagonist. Ro 41-5253 can bind RARα without inducing transcription or affecting RAR/RXR heterodimerization and DNA binding. Ro 41-5253 can inhibit cancer cell proliferation and induce apoptosis, has antitumor activity .
    Ro 41-5253
  • HY-15128


    RAR/RXR Apoptosis Endogenous Metabolite Neurological Disease Inflammation/Immunology Cancer
    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 .
    9-cis-Retinoic acid
  • HY-132334S

    RAR/RXR Apoptosis Neurological Disease Inflammation/Immunology Cancer
    9-cis-Retinoic acid-d5 is the deuterium labeled 9-cis-Retinoic acid. 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[1][2][3][4][5][6].
    9-cis-Retinoic acid-d5
  • HY-125904

    RAR/RXR Neurological Disease Inflammation/Immunology Cancer
    4-Hydroxyretinoic acid (4-HRA) is a naturally occurring retinoid derivative with diverse biological effects. 4-Hydroxyretinoic acid is formed from retinol catalyzed by cytochrome P-450 isozyme(s), and is mainly metabolized by the liver in the body. 4-Hydroxyretinoic acid also serves as the substrate for human liver microsomal UDP-glucuronosyltransferase(s) and recombinant UGT2B7. 4-Hydroxyretinoic acid regulates gene expression and cell differentiation via binding to nuclear receptor RAR (Retinoic Acid Receptor), and activates RARs and RXR-alpha, to induce cancer cell apoptosis. In addition, 4-Hydroxyretinoic acid is also involved in various physiological processes such as immune regulation, neuroprotection, and anti-oxidation .
    4-Hydroxyretinoic acid
  • HY-100008
    3 Publications Verification


    RAR/RXR SphK Autophagy HCV Infection Cancer
    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 . 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 .

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