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RAR Agonist
DC271 is a potent RAR agonist that functions as a retinoid, stimulating cellular responses similar to those of endogenous retinoic acid (ATRA) and the synthetic retinoid EC23. By binding to retinoid protein machinery such as CRABPII, DC271 facilitates the translocation of ATRA into the nucleus, enhancing retinoid signaling pathways. This compound is valuable for research applications involving gene expression regulation, differentiation, and cellular growth in various biological contexts. -
RAR Agonist
MDI-403 is a highly potent retinoic acid receptor (RAR) agonist, exhibiting an EC50 value of less than 1 μM. It demonstrates significant antiviral activity against SARS-CoV-2 by dose-dependently inhibiting the expression of viral nucleoprotein (NP) and decreasing the proportion of infected cells, mainly during the virus invasion stage. MDI-403 serves as a valuable tool for research focused on the mechanisms of antiviral activity and potential therapies against SARS-CoV-2. -
RXR Agonist
MSU-42011 is an orally active retinoid X receptor (RXR) agonist that demonstrates significant immunomodulatory and antitumor properties. This compound effectively inhibits inducible nitric oxide synthase (iNOS) activity and downregulates the expression of phosphorylated extracellular signal-regulated kinase (p-ERK) protein. MSU-42011 is a valuable tool for research applications focused on cancer biology and immunology. -
RARβ/RARα Antagonist
LE135 is a selective antagonist of retinoic acid receptors RARα and RARβ, exhibiting a Ki of 1.4 μM for RARα and a significantly higher affinity of 220 nM for RARβ. This compound demonstrates high specificity for these targets, with minimal interaction with RARγ and RXR isoforms. Additionally, LE135 acts as a potent activator of TRPV1 and TRPA1 receptors, with EC50 values of 2.5 μM and 20 μM, respectively, making it a valuable tool for studying pathways involving these ion channels in various biological contexts. -
Inverse RAR Inhibitor
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. -
Retinol Derivative
Hydroxypinacolone retinoate (HPR) is a retinol derivative that selectively binds to retinoic acid receptors (RARs). Its primary biological activity includes promoting cellular turnover and collagen synthesis, making it relevant in anti-aging research. HPR is often studied for its potential to improve skin texture and reduce the appearance of fine lines and wrinkles, particularly when used in conjunction with other retinoids. -
RAR Antagonist
AGN 193109 is a potent retinoic acid receptor (RAR) antagonist, exhibiting binding affinities of 2 nM, 2 nM, and 3 nM for RARα, RARβ, and RARγ, respectively. This compound is utilized in research to investigate RAR signaling and its implications in various biological processes. Additionally, AGN 193109 contains an alkyne group that enables its use in click chemistry applications through copper-catalyzed azide-alkyne cycloaddition (CuAAc). Its therapeutic potential includes serving as an antidote for retinoic acidosis, alleviating skin and mucosal toxicity associated with excess retinoic acid. -
RXR-Selective Agonist
SR11237 is a potent retinoid X receptor (RXR)-selective agonist that exhibits no activity on retinoic acid receptors (RARs). This compound efficiently induces the formation of RXR/RXR homodimers and effectively transactivates reporter genes containing RXR-responsive elements. It is valuable for research in areas related to nuclear hormone signaling pathways and RXR-mediated transcriptional regulation. -
RAR-α/RAR-β Agonist
Ch55 is a potent agonist of the retinoic acid receptors RAR-α and RAR-β. It demonstrates a high affinity for these receptors while exhibiting low binding affinity for cellular retinoic acid binding protein (CRABP). Ch55 effectively induces differentiation in HL60 cells, with an EC50 of 200 nM. This compound is particularly valuable in cancer research applications, offering insights into retinoid-mediated pathways in tumorigenesis and cell differentiation. -
RXR Agonist
CD3254 is a potent and selective retinoid-X-receptor (RXR) agonist that plays a crucial role in modulating gene expression related to lipid metabolism, apoptosis, and differentiation. Its activation of RXR can influence signaling pathways involved in various diseases, making it a valuable tool for research in metabolic disorders and cancer. CD3254 is suitable for studies investigating RXR's role in cellular processes and its potential therapeutic applications. -
RARγ Antagonist
MM11253 is a potent and selective antagonist of Retinoic Acid Receptor gamma (RARγ) with an IC50 of 44 nM. It exhibits minimal activity against RARα, RARβ, and RXRα. This compound effectively inhibits the growth-promoting effects of RARγ-selective agonists, making it a valuable tool for research focused on cancer biology and metabolism involving RARγ signaling pathways. -
RXR Antagonist
PA452 is a specific antagonist of the retinoic X receptor (RXR). It effectively inhibits the actions of retinoic acid (RA) on the differentiation of Th1 and Th2 cells. This compound is relevant for research focusing on immune response modulation and the therapeutic potential in various inflammatory and autoimmune conditions. -
RARα Agonist
BMS 753 is an isotype-selective retinoic acid receptor α (RARα) agonist, exhibiting a Ki of 2 nM. This compound modulates gene expression linked to cellular differentiation, proliferation, and apoptosis through RARα activation. Its selective action makes BMS 753 valuable for investigating the role of RARα in various biological processes and potential therapeutic areas, including cancer research and regenerative medicine. -
RAR-beta/gamma Antagonist
CD2665 is a selective antagonist of retinoic acid receptors RAR-β and RAR-γ, exhibiting Kd values of 306 nM and 110 nM for each receptor, respectively. This compound is beneficial for studying the modulation of retinoic acid signaling pathways implicated in various biological processes. CD2665 is suitable for applications in cancer research, developmental biology, and pharmacological studies involving retinoid signaling. -
RARβ agonist
CD2314 is a potent and selective agonist of the RARβ receptor, exhibiting a Kd of 195 nM in S91 melanoma cells. This compound modulates retinoic acid signaling pathways, promoting cellular differentiation and apoptosis. CD2314 is valuable for investigating the roles of RARβ in cancer biology and other research applications related to retinoid signaling. -
RXR Modulater
LG100754 is an RXR modulator that functions as an antagonist of RXR:RXR homodimers while acting as an agonist for RXR:PPARα and RXR:PPARγ heterodimers. This compound serves as an insulin sensitizer, exerting its biological effects through receptor interactions involving the retinoid X receptor (RXR). Its unique modulation of RXR dimers makes LG100754 a valuable tool for research in metabolic disorders and cellular signaling pathways. -
RARα Antagonist
ER 50891 is a RARα antagonist that counteracts the inhibitory effects of all-trans retinoic acid (ATRA) on metabolic activity and proliferation in MC3T3-E1 preosteoblasts. This compound effectively rescues ATRA-reduced osteocalcin (OCN) expression and enhances extracellular matrix mineralization, while simultaneously suppressing alkaline phosphatase (ALP) activity. ER 50891 is applicable for research focused on osteoporosis and the mechanisms of ATRA-induced inhibition of osteoblastogenesis. -
RARβ Agonist
BMS641 is a selective RARβ agonist with a high affinity for the RARβ receptor (Kd of 2.5 nM), exhibiting over 100-fold selectivity compared to RARα (Kd of 225 nM) and RARγ (Kd of 223 nM). This compound is valuable in investigating the role of RARβ in various biological processes and may have implications in cancer research and differentiation studies. Its specificity makes BMS641 a useful tool for elucidating RARβ-mediated signaling pathways. -
RARβ2 Agonist
KCL-286 is a potent retinoic acid receptor (RAR) β2 agonist, with an EC50 of 1.9 nM, demonstrating high selectivity over RAR α and RAR γ (EC50 = 26 nM and 11 nM, respectively). This compound activates RARβ2 specifically in injured neurons, promoting axonal regeneration in the spinal cord and sensory nerves by altering the inhibitory environment in the central nervous system. KCL-286 also modulates neuroinflammation and extracellular matrix components, influencing the expression of chondroitin sulfate proteoglycans through neuronal secretion of decorin to facilitate myelination and enhance axonal growth. It is relevant for research applications in spinal cord injury and traumatic nerve injury studies. -
RARbeta2 Agonist
AC-261066 is a selective agonist of the retinoic acid receptor beta2 (RARbeta2) with high potency and oral bioavailability, exhibiting a pEC50 of 8.0. This compound is utilized in research to investigate the biological functions of RARbeta2 and its implications in cellular differentiation, growth, and apoptosis. Its isoform-selective action makes it a valuable tool for studies aimed at understanding retinoid signaling pathways and their therapeutic potential. -
RXR Agonist
HX600 is a synthetic agonist targeting the retinoid X receptor (RXR) heterodimer complex. It demonstrates neuroprotective properties by preventing ischemia-induced neuronal damage, making it valuable for research into neurodegenerative disorders and ischemic injury. Additionally, HX600 exhibits oral bioavailability, enhancing its potential for in vivo studies. -
RXRα Antagonist
XS-060 is a potent RXRα antagonist that functions by disrupting the interaction between phosphorylated RXRα (pRXRα) and PLK1, leading to RXRα-dependent mitotic arrest. This compound specifically targets the centrosomal interaction of p-RXRα and PLK1 without interfering with RXRα heterodimerization with RARγ. XS-060 is primarily utilized in cancer research to explore mechanisms of mitotic regulation and potential therapeutic applications in oncology. -
RARγ Agonist
BMS961 is a selective agonist of the retinoic acid receptor-γ (RARγ). It demonstrates potent anti-inflammatory activity, making it a valuable tool for research into inflammatory diseases and related pathways. This compound can be utilized in studies aimed at understanding RARγ-mediated signaling and its implications in therapeutic contexts. -
RAR Neutral Antagonist
AGN 192870 is a selective RAR neutral antagonist that demonstrates binding affinities (Kd) of 147 nM for RARα, 33 nM for RARβ, and 42 nM for RARγ. It exhibits inhibitory concentrations (IC50) of 87 nM for RARα and 32 nM for RARγ while showcasing partial agonism at RARβ. Additionally, AGN 192870 features an alkyne group, facilitating its use as a click chemistry reagent through copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, providing utility in various chemical biology applications. -
Nuclear Retinoic Acid Receptor γ Inhibitor
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. -
RARα Antagonist
RARα antagonist 1 is a selective antagonist of the retinoic acid receptor α (RARα), functioning at an IC50 of 4.6 nM. This compound disrupts RARα-mediated signaling, making it a valuable tool for studying the role of this receptor in various biological processes. Its applications extend to cancer research, developmental biology, and investigations of metabolic disorders, where modulation of retinoic acid signaling is crucial. -
Retinoid X Receptor Modulator
RXR Antagonist 1 is a selective retinoid X receptor (RXR) modulator demonstrating potent antagonistic activity, with a pA2 value of 8.06. This compound is particularly relevant in research pertaining to type 2 diabetes, offering insights into RXR-related pathways and their impact on metabolic processes. Its effective inhibition of RXR activity makes it a valuable tool for exploring therapeutic interventions in metabolic disorders. -
RAR/RXR Inhibitor
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. -
RARγ Nuclear Receptor Agonist
IRX5010 is a selective agonist of the RARγ nuclear receptor. It has been shown to inhibit the in vivo growth of EMT-6 triple-negative breast cancer cells, making it a valuable tool for cancer research. This compound is particularly useful for studying the role of RARγ in tumor biology and exploring therapeutic strategies targeting this receptor. -
RARs Agonist
Arotinoid functions as a highly potent agonist of retinoic acid receptors (RARs). Known for its antipsoriatic effects, Arotinoid exhibits antipapilloma activity with an ED50 of 0.05 mg/kg. This compound is valuable in research related to skin carcinomas, contributing to the understanding of retinoid biology and potential therapeutic applications. -
RAR/RXR Agonist
Fluorobexarotene is a potent agonist of retinoid-X-receptors (RXR), exhibiting a Ki value of 12 nM and an EC50 value of 43 nM for the RXRα receptor. This compound demonstrates a binding affinity for RXR that is 75% greater than that of Bexarotene. Fluorobexarotene is valuable for research applications targeting RXR-mediated signaling pathways, which are implicated in various biological processes including cellular differentiation and metabolism. -
RAR/RXR Activator
Viaminate is a potent RAR/RXR activator, functioning as a derivative of Retinoic acid. It plays a crucial role in regulating gene expression involved in cellular differentiation and proliferation. This compound is primarily utilized in research on severe acne and various keratinization disorders, providing insights into the underlying molecular mechanisms and potential therapeutic avenues. -
RXR Agonist
16α-Hydroxytrametenolic acid is a natural triterpene that selectively functions as an agonist for the retinoid X receptor (RXR). This compound has demonstrated potential in modulating RXR activity, thereby influencing pathways involved in lipid metabolism, cell differentiation, and apoptosis. Its applications in research include studying RXR's role in cancer biology and metabolic disorders, providing valuable insights into therapeutic approaches targeting these pathways. -
RAR/RXR Inhibitor
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. -
Retinoic Acid Analogue
DC360 is a synthetic retinoid analogue of all-trans retinoic acid (ATRA) that primarily targets retinoic acid receptors (RARs), particularly RARβ. It plays a significant role in modulating gene expression and is instrumental in the study of retinoid signaling pathways. Researchers can utilize DC360 to explore its effects on cellular differentiation and proliferation in various biological contexts. -
Retinoic Acid Receptor Agonist
ALRT1550 is a potent selective agonist of the retinoic acid receptors (RARs), exhibiting Kd values between 1-4 nM. This compound demonstrates significant anti-proliferative effects, evidenced by an IC50 of 0.22 nM in UMSCC-22B squamous carcinoma cells. In vivo studies in mouse tumor xenograft models have shown ALRT1550 to inhibit tumor growth in a dose-dependent manner, achieving up to 89% inhibition at maximum doses. This reagent is highly relevant for research focused on cancer biology and therapeutic applications targeting the retinoic acid signaling pathway. -
RXR Antagonist
RXR Antagonist 2 is a potent antagonist of retinoid X receptors (RXR), exhibiting a Ki value of 0.391 μM and a Kd of 0.281 μM. This compound is valuable for investigating RXR-related biological processes and diseases, making it a useful tool in molecular biology and pharmacological research. Its ability to inhibit RXR activity allows for studies on its role in various signaling pathways and therapeutic interventions. -
RXR Agonist
NEt-iFQ is a fluorescent retinoid X receptor (RXR) agonist that exhibits potent solvatochromic properties. This compound selectively binds to the RXR-ligand binding pocket, producing fluorescence, which facilitates studies on RXR-mediated signaling pathways. It is useful in research applications involving nuclear receptor activation and cellular imaging. -
RAR Antagonist
AGN 193109 sodium is a potent pan antagonist of retinoic acid receptors (RAR), specifically targeting RARα, RARβ, and RARγ with dissociation constants (Kd) of 2, 2, and 3 nM, respectively. This compound effectively reverses morphology changes induced by TTNPB and alleviates the proliferation suppression caused by all-trans retinoic acid, 9-cis RA, and 13-cis RA in ECE16-1 cells. Additionally, AGN 193109 sodium serves as an antidote for retinoic acidosis, mitigating skin and mucosal toxicity associated with retinoid treatment. -
Nurr1-RXRα Activator
BRF110 is a selective, orally active rexinoid that targets the Nurr1-Retinoid X Receptor alpha (RXRα) heterodimer, exhibiting an EC50 of 0.9 μM in SH-SY5Y cells. This compound upregulates brain-derived neurotrophic factor (BDNF) expression and demonstrates neuroprotective effects against MPP+-induced toxicity. Notably, BRF110 is capable of crossing the blood-brain barrier, making it a valuable tool for research in neurobiology and potential therapeutic applications in neurodegenerative diseases. -
RXR Modulator
LG101506 is a selective and orally active retinoid X receptor (RXR) modulator that exhibits a Ki of 2.7 nM for RXRα. This compound has demonstrated potential in research applications related to type 2 diabetes and cancer, making it a valuable tool for studying RXR's role in metabolic and oncological pathways. -
Retinoid Agonist
ER-38925 is a selective retinoid agonist targeting retinoic acid receptor subtype α (RAR-α). This compound demonstrates a dose-dependent ability to prolong the lifespan of recipient mice and effectively inhibits alloantigen-stimulated donor T lymphocyte proliferation in vitro. Additionally, ER-38925 can prevent the development of antiallogeneic cytotoxic T lymphocyte responses and suppress serum anti-DNA autoantibody production in mouse models of human chronic graft-versus-host disease (GVHD). Its unique properties make it a valuable tool for research in immunological responses and therapy development. -
Retinoic Acid Receptor Antagonist
LE-540 is a selective antagonist of the retinoic acid receptor beta (RARβ), with a reported inhibition constant (Ki) of 0.22 μM. This compound demonstrates significant potential in cancer research, specifically in the study of breast cancer and lung cancer. Through its ability to modulate RARβ activity, LE-540 can provide valuable insights into retinoid signaling pathways and their implications in tumorigenesis. -
RAR/RXR Agonist
5,6-Epoxyretinoic acid acts as an agonist for all isoforms of retinoic acid receptors (RAR), demonstrating EC50 values of 77 nM, 35 nM, and 4 nM for RARα, RARβ, and RARγ, respectively. This compound exhibits notable growth arrest in MCF-7 and NB4 cell lines at a concentration of 1 μM. As a natural metabolite of all-trans retinoic acid, which derives from vitamin A, 5,6-epoxyretinoic acid plays a significant role in various cellular processes and research applications related to cancer biology and retinoid signaling pathways. -
RAR/RXR Activator
TBTC is a selective retinoic acid receptor (RAR) and retinoid X receptor (RXR) activator. It demonstrates notable effects in improving behavioral deficits in Alzheimer's disease model mice, enhancing the activation of heterodimers formed by RXRα with LXRα or PPARγ. TBTC promotes the expression of key genes including apoE, ABCA1, and ABCG1, while effectively reducing amyloid-beta (Aβ) levels in cellular and animal studies, making it a valuable tool for Alzheimer’s research. -
RARγ Activator
NRX-204647 is a selective retinoic acid receptor gamma (RARγ) activator that exhibits high specificity compared to RARα and RARβ. This compound demonstrates significant biological activity in inhibiting bone formation, as evidenced by its ability to reduce bone volume/tissue volume (BV/TV). NRX-204647 is a valuable tool for investigating mechanisms in anti-cancer research and elucidating the role of RARγ in various biological processes. -
RXR/RAR Agonist
AGN-191659 is a potent agonist of retinoid X receptors (RXR) and retinoic acid receptors (RAR), exhibiting EC50 values of 11 nM, 23 nM, and 37 nM for RXRα, RARβ, and RARγ, respectively. It enhances gene transcription through activation of these receptors and has demonstrated significant biological activities, including the induction of tissue transglutaminase and suppression of chondrogenesis. Additionally, AGN-191659 effectively reverses fibroblast growth factor-induced endothelial cell proliferation and inhibits heparin-releasable lipase activity. This compound is valuable for research related to promyelocytic leukemia and hypertriglyceridemia. -
RARβ Agonist
BMS-948 is a selective agonist of the retinoic acid receptor beta (RARβ), exhibiting an EC50 of 0.1 µM. This compound plays a significant role in the modulation of gene expression related to tumor progression, embryonic development, and tissue remodeling. It serves as a valuable tool for investigating the biological functions of RARβ in various research applications. -
RXRα Agonist
GW0791 is an RXRα agonist with an EC50 of 5 nM. This compound demonstrates significant biological activity in modulating retinoid signaling pathways, making it a valuable tool for cancer research. Its ability to activate RXRα offers potential insights into mechanisms of tumorigenesis and opportunities for therapeutic development. -
RXR Agonist
(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.

