Retinoid Receptor

Cat. No.

A77470

CAS No.

262433-54-5

BMS270394

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.

Cat. No.

A77471

CAS No.

3053403-01-0

RARα antagonist 1

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.

Cat. No.

A77472

CAS No.

3010910-40-1

RXR antagonist 1

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.

Cat. No.

A77473

CAS No.

1807740-94-8

RXR antagonist 5

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.

Cat. No.

A77474

CAS No.

856683-59-5

IRX5010

Synonyms: IRX4647F

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.

Cat. No.

A77475

CAS No.

71441-09-3

Arotinoid

Synonyms: Ro 13-6298; Arotinoid ethyl ester

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.

Cat. No.

A77476

CAS No.

1190848-23-7

Fluorobexarotene

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.

Cat. No.

A77477

CAS No.

53839-71-7

Viaminate

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.

Cat. No.

A77478

CAS No.

176390-68-4

16α-Hydroxytrametenolic acid

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.

Cat. No.

A77479

CAS No.

2367641-24-3

NBD-125

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.

Cat. No.

A77481

CAS No.

2324152-25-0

DC360

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.

Cat. No.

A77482

CAS No.

178600-20-9

ALRT1550

Synonyms: LGD1550

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.

Cat. No.

A77483

CAS No.

3010910-41-2

RXR antagonist 2

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.

Cat. No.

A77484

CAS No.

1251538-60-9

NEt-iFQ

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.

Cat. No.

A77485

CAS No.

2319838-82-7

AGN 193109 sodium

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.

Cat. No.

A77486

CAS No.

2095489-35-1

BRF110

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.

Cat. No.

A77487

CAS No.

331248-11-4

LG101506

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.

Cat. No.

A77488

CAS No.

196517-43-8

ER-38925

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.

Cat. No.

A77489

CAS No.

188645-44-5

LE-540

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.

Cat. No.

A77490

CAS No.

13100-69-1

5,6-Epoxyretinoic acid

Synonyms: 5,6-epoxy atRA; 5,6-epoxy RA

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.

Cat. No.

A77491

CAS No.

213192-26-8

TBTC

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.

Cat. No.

A77492

CAS No.

1351452-80-6

NRX-204647

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.

Cat. No.

A77493

CAS No.

156691-86-0

AGN-191659

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.

Cat. No.

A77494

CAS No.

168901-49-3

BMS-948

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.

Cat. No.

A77495

CAS No.

503620-39-1

GW0791

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.