Retinoid Receptor

Cat. No.

A39746

CAS No.

925701-88-8

Acitretin sodium

Synonyms: Ro 10-1670 sodium

Acitretin sodium functions as a retinoic acid receptor (RAR) and retinoid X receptor (RXR) agonist. Primarily utilized in the treatment of psoriasis, this second-generation systemic retinoid also shows potential in the research of Alzheimer's disease. Its ability to modulate gene expression and influence cellular differentiation makes it a valuable tool for investigating retinoid signaling pathways in various biological contexts.

Cat. No.

A45007

CAS No.

198696-03-6

DC271

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.

Cat. No.

A53357

CAS No.

127471-94-7

MDI-403

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.

Cat. No.

A65099

CAS No.

2456434-36-7

MSU-42011

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.

Cat. No.

A68699

CAS No.

155877-83-1

LE135

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.

Cat. No.

A77450

CAS No.

215030-90-3

BMS493

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.

Cat. No.

A77451

CAS No.

893412-73-2

Hydroxypinacolone retinoate

Synonyms: HPR

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.

Cat. No.

A77452

CAS No.

171746-21-7

AGN 193109

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.

Cat. No.

A77453

CAS No.

146670-40-8

SR11237

Synonyms: BMS-649

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.

Cat. No.

A77454

CAS No.

110368-33-7

Ch55

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.

Cat. No.

A77455

CAS No.

196961-43-0

CD3254

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.

Cat. No.

A77456

CAS No.

345952-44-5

MM11253

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.

Cat. No.

A77457

CAS No.

457657-34-0

PA452

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.

Cat. No.

A77458

CAS No.

215307-86-1

BMS 753

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.

Cat. No.

A77459

CAS No.

170355-78-9

CD2665

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.

Cat. No.

A77460

CAS No.

170355-37-0

CD2314

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.

Cat. No.

A77461

CAS No.

180713-37-5

LG100754

Synonyms: UVI 2112

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.

Cat. No.

A77462

CAS No.

187400-85-7

ER 50891

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.

Cat. No.

A77463

CAS No.

369364-50-1

BMS641

Synonyms: BMS-209641

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.

Cat. No.

A77464

CAS No.

1952276-71-9

KCL-286

Synonyms: C286

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.

Cat. No.

A77465

CAS No.

870773-76-5

AC-261066

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.

Cat. No.

A77466

CAS No.

172705-89-4

HX600

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.

Cat. No.

A77467

CAS No.

346721-50-4

XS-060

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.

Cat. No.

A77468

CAS No.

185629-22-5

BMS961

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.

Cat. No.

A77469

CAS No.

166977-57-7

AGN 192870

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.