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Retinoid receptor ligands act on retinoic acid receptors (RARs) and retinoid X receptors (RXRs). Both are nuclear receptors with α, β and γ subtypes that bind DNA as RAR-RXR heterodimers and regulate gene transcription. A receptor for the morphogen retinoic acid was identified in 1987 as a member of the nuclear receptor family. In 1990 a second receptor responding to retinoic acid, later named RXRα, revealed a distinct retinoid pathway. Tretinoin, the all-trans form of retinoic acid, activates RARs, while tamibarotene and AM 580 favor RARα and CD 437 favors RARγ. Adapalene, tazarotene, acitretin and fenretinide are synthetic retinoids, whereas bexarotene is a ligand selective for RXRs.
Synonyms: UAB30
(all-E)-UAB30 is a selective agonist of the retinoid X receptor (RXR). It demonstrates significant anti-proliferative activity in MyLa, HuT 78, and HH cell lines, with IC50 values of 34.7 μM, 5.1 μM, and 22.4 μM, respectively. This compound is valuable for research focused on cancer biology and RXR signaling pathways, providing insights into cell growth regulation.
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Nurr1/RXR Agonist 1 is a dual agonist that specifically targets the Nurr1 receptor (EC50 = 2.6 µM) and retinoid X receptor (RXR) with affinity constants of 0.6 and 1.1 µM, respectively. This compound selectively activates the DR5 response element by destabilizing the Nurr1 homodimer while stabilizing the Nurr1:RXR heterodimer. Nurr1/RXR Agonist 1 promotes the expression of neuroprotective target genes while minimizing off-target effects in neuronal cells. This reagent is suitable for research in neurodegenerative diseases.
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JP3000 is a potent agonist of retinoic acid receptors RARA, RARB, and RARG. This compound is designed to modulate gene expression involved in cellular differentiation, development, and homeostasis. Its applications in research include investigating the molecular mechanisms of retinoid signaling in various biological processes and disease states, making it a valuable tool for exploring therapeutic strategies in cancer and metabolic disorders.
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CU-6PMN is a fluorescent retinoid X receptor (RXR) agonist that selectively activates human RXRα with an EC50 value of 22 nM and a Ki value of 230 nM. This compound exhibits a maximum absorption wavelength of 396 nm and an emission wavelength of 453 nm when dissolved in 0.1 N NaOH aqueous solution. CU-6PMN is valuable for research applications involving RXR ligand screening and provides a useful tool for studying RXR-mediated biological processes.
Seletinoid G is a potent retinoic acid receptor (RAR) agonist. It demonstrates significant biological activity by promoting the repair of altered connective tissue in aged skin while inhibiting UV-induced collagen deficiency in younger skin. This compound is valuable for research applications focused on skin aging and photoaging, facilitating the exploration of therapeutic strategies for improving skin health and resilience.
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