Home Metabolism Retinoid Receptor

Retinoid Receptor Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S5233 Fenretinide Fenretinide is a synthetic derivative of retinoic acid that has a broad-spectrum of cytotoxic activity against primary tumor cells, cell lines, and/or xenografts of various cancers (including neuroblastoma). This compound (4-hydroxy(phenyl)retinamide; 4-HPR) is a synthetic derivative of retinoic acid, and it can bind to retinoic acid receptor (RAR) and retinoid X receptor (RXR) at concentrations necessary to induce cell death.
iScience, 2024, 27(10):110862
Acta Pharm Sin B, 2023, 13(1):142-156
E1627 BMS493 BMS493 is an inverse agonist of pan retinoic acid receptor (RAR). It increases nuclear corepressor interaction with RARs and can be used as an inhibitor for the dietary and pharmacologic manipulation of retinoic acid (RA) activity in vivo and in vitro.
bioRxiv, 2025, 2025.05.16.653860
S6605 AR7 AR7 is a retinoic acid receptor α (RARα) antagonist. This compound is a potent and selective inhibitor of RARα, demonstrating high affinity and specificity for this receptor subtype. It effectively blocks the binding of retinoic acid to RARα, thereby inhibiting downstream signaling pathways. In cellular assays, this chemical has been shown to suppress the proliferation of various cancer cell lines that are dependent on RARα signaling. Additionally, it induces apoptosis in these cells, highlighting its potential as a therapeutic agent. The pharmacological profile of this antagonist supports its use in studying RARα-mediated processes and in developing treatments for related diseases.
Phytomedicine, 2024, 136:156286
S4699 Etretinate Etretinate (Tegison, Ethyl etrinoate, Retinoid, Etretinato,Ro 10-9359) is an oral aromatic retinoid acid which is effective in psoriasis and other dermatological syndromes. It activates retinoid receptors, causing an induction of cell differentiation, inhibition of cell proliferation, and inhibition of tissue infiltration by inflammatory cells.
Viruses, 2021, 13(8)1533
E1445 Palovarotene Palovarotene (R 667; Ro 3300074) is a nuclear retinoic acid receptor γ (RAR-γ) agonist. It reduces heterotopic ossification (HO) in cultures and in murine and rat fibrodysplasia ossificans progressiva (FOP) models.
E6408New CD1530 CD1530 is a potent and selective agonist of RARγ receptor with Ki values of 150 nM. It is a potent inhibitor of heterotopic ossification (HO) and may be effective against congenital HO, with potential use in research on psoriasis, acne, photoaging, and cancer.
E4618 CD3254 CD3254 is a potent and selective agonist of retinoid X receptor (RXR). It may be utilized in cancer research and holds promise for the treatment of metabolic diseases.
E1695 9-cis-Retinoic acid 9-cis-Retinoic acid (Alitretinoin, ALRT 1057) is an active metabolite of vitamin A that functions as a high-affinity ligand for retinoid X receptors (RXRs) and also activates retinoic acid receptors (RARs). It inhibits adipogenesis by activating RXR while simultaneously decreasing RXRα and PPARγ levels in an RXR activation-independent manner.
E1767New HX531 HX531 is an orally active antagonist of RXR. This compound enhances activation of the p53–p21Cip1 pathway and abrogates the anti-apoptotic effects of all-trans-retinoic acid (t-RA). It exhibits anti-obesity, anti-diabetic, and anti-melanoma properties.
S6132 All trans-Retinal All trans-Retinal (Retinaldehyde, Vitamin A aldehyde, Retinene), a component of the retinoid cycle, is converted to retinoic acid in vivo by the action of retinal dehydrogenase. Retinoic acid is a ligand for both RAR and RXR. All trans-retinal ias a potent photosensitizer.
S2520 CD437(AHPN) CD437(AHPN), a synthetic retinoid, is a selective Retinoic acid Receptor γ ( RARγ) agonist. It exhibits an antiproliferative effect and induces apoptosis via activation of AP-1 in vitro.
E1468 MSU-42011 MSU-42011 is an orally active agonist of retinoid X receptor (RXR). This compound inhibits the expression of iNOS and p-ERK protein. It exhibits immunomodulatory and antitumor activity. It can be used for cancer research.
E7548 Ch55 Ch55 is a synthetic analog of retinoic acid that acts as a potent agonist of RAR, binding with high affinity to retinoic acid receptors RAR-α, RAR-β, and RAR-γ, while showing no binding to cellular retinoic acid binding protein (CRABP). It demonstrates anti-fibrotic effects in preclinical models, reducing collagen deposition and hypertrophy in dermal tissues.