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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: R115866
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.
(+)-Talarozole is a potent inhibitor of retinoic acid metabolism extracted from patent WO 1997049704 A1.
(-)-Talarozole is a potent inhibitor of retinoic acid metabolism extracted from patent WO 1997049704 A1.
ZSH-512 is a potent inhibitor of retinoic acid receptor gamma (RARγ). It demonstrates significant antiproliferative effects by inducing apoptosis in cancer cells, while concurrently downregulating key stemness markers such as CD133, NANOG, SOX2, and EPCAM. With its strong anticancer activity, ZSH-512 is a valuable tool for investigating therapeutic strategies in colorectal cancer research.
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BMS493 is an inverse pan-retinoic acid receptor (RAR) agonist that enhances nuclear corepressor interaction with RARs, effectively inhibiting retinoic acid-induced differentiation. This compound serves as a valuable tool in research applications focused on RAR signaling pathways and their regulatory mechanisms. Additionally, BMS493 features an alkyne group, enabling its use in click chemistry through copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, facilitating diverse labeling and conjugation strategies.
BMS270394 is a selective inhibitor of the nuclear retinoic acid receptor gamma (RAR-γ), exhibiting an EC50 of 30 nM for human RAR-γ. This compound demonstrates potent activity against RAR-β with an EC50 of 400 nM. BMS270394 is valuable in research applications focused on gene regulation, developmental biology, and potential therapeutic interventions related to retinoid signaling pathways.
RXR Antagonist 5 is a selective retinoic acid X receptor (RXR) inhibitor, designed to modulate RXR activity. It effectively disrupts RXR signaling pathways, making it a valuable tool for investigating the role of RXR in various biological processes. This compound can be utilized in research applications focused on cancer biology, metabolism, and developmental studies, providing insights into RXR-mediated physiological functions.
NBD-125 is a potent RAR/RXR inhibitor that modulates retinoic acid receptor signaling. It functions as an RXRα activator, demonstrating an IC50 of 31.10 μM in KM12C cells. This compound is valuable for research applications involving the regulation of gene expression and signaling pathways associated with nuclear receptor activity.
AGN 191701 is a selective retinoic acid receptor (RAR) and retinoid X receptor (RXR) inhibitor. This compound has been shown to induce liver enlargement in rat models while preserving hepatocellular integrity, indicating a unique biological profile. AGN 191701 serves as a valuable tool for studying retinoid signaling pathways and their implications in hepatic processes.
