RAR/RXR Inhibitor

Cochinchinone P is a retinoid X receptor-α (RXRα) inhibitor that inhibits 9-cis-retinoic acid (HY-15128)-induced transcriptional activity of RXRα in vitro. Cochinchinone P can be used in cancer research.

R-116010 is a potent and selective retinoic acid (RA) metabolism inhibitor and can inhibit hydroxylase CYP26. R-116010 can enhance the anti-tumor effect of retinoic acid drugs. R-116010 can be used for the research of cancer, metabolic and neurological disease, such as neuroblastoma.

Tarenflurbil (Standard) is the analytical standard of Tarenflurbil. This product is intended for research and analytical applications. Tarenflurbil ((R)-Flurbiprofen) is the R-enantiomer of the racemate NSAID Flurbiprofen, Tarenflurbil ((R)-Flurbiprofen) inhibits the binding of [3H]9-cis-RA to RXRα LBD with IC50 of 75 μM. Tarenflurbil can be used for Alzheimer's disease research.

SR11237 GMP is SR11237 (HY-107413) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. SR11237 is a RXR activator and lipid metabolism regulator that promotes the differentiation of induced neural stem cells into dopaminergic (TH-positive) neurons. SR11237 induces transcriptional regulation of lipogenic genes and cholesterol transporters, increases glycosaminoglycan release, and elevates total cellular triglyceride levels. SR11237 promotes heterodimerization of RXR with Nurr1, thereby enhancing tyrosine hydroxylase expression and facilitating dopamine release. SR11237 produces a synergistic effect when used in combination with bFGF/EGF. SR11237 is mainly used in studies related to osteoarthritis and Parkinson's disease.

Sampsonione P is an RXRα inhibitor isolated and extracted from Hypericum sampsonii. Sampsonione P inhibits RXRα transcriptional activity and can downregulate the expression of pro-inflammatory proteins such as iNOS and COX-2, thereby exerting anti-inflammatory effects. Sampsonione P has antitumor activity. Sampsonione P can be used for research on inflammatory diseases and cancer.

SR210831C is a highly selective, orally active retinoic acid receptor α (RARα) inhibitor with an IC₅₀ of 0.051 nM. SR210831C suppresses spermatogenesis by reducing sperm count in house mice via acting on the early stages of spermatogenesis, and it does not cross the blood-testis barrier. SR210831C can be used in male contraception research.

Fenretinide (Standard) is the analytical standard of Fenretinide. This product is intended for research and analytical applications. Fenretinide (4-HPR) is a synthetic retinoid deriverative, binding to the retinoic acid receptors (RAR) at concentrations necessary to induce cell death.

AGN 191701 is a selective retinoic acid X receptor (RXR) agonist that causes liver enlargement in rats without hepatocellular necrosis.

Nurr1/RXR dual agonist 1 is a dual activator of Nurr1 (EC₅₀ = 2.6 µM) and RXR with Ks of 0.6 and 1.1 µM, respectively. Nurr1/RXR dual agonist 1 exclusively activates the heterodimer response element DR5 by selectively destabilizing the Nurr1 homodimer and stabilizing the Nurr1:RXR heterodimer. Nurr1/RXR dual agonist 1 enhances expression of a specific subset of neuroprotective Nurr1 target genes while avoiding induction of genes associated with potential off-target effects in neuronal cells. Nurr1/RXR dual agonist 1 can be used for neurodegenerative diseases research.

BMS493 (Standard) is the analytical standard of BMS493 (HY-108529). This product is intended for research and analytical applications. BMS493 is an inverse pan-retinoic acid receptor (RAR) agonist. BMS493 increases nuclear corepressor interaction with RARs. BMS493 also could prevent retinoic acid-induced differentiation. BMS493 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

UVI 3003 (Standard) is the analytical standard of UVI 3003 (HY-107500). This product is intended for research and analytical applications. UVI 3003 is a highly selective antagonist of retinoid X receptor (RXR), and inhibits xenopus and human RXRα in Cos7 cells, with IC₅₀s of 0.22 and 0.24 μM, respectively.

Liarozole (dihydrochloride) (Standard) is the analytical standard of Liarozole (dihydrochloride). This product is intended for research and analytical applications. Liarozole (R75251) dihydrochloride is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole dihydrochloride inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of RA (IC50=7 μM), resulting in increased tissue levels of RA. Liarozole dihydrochloride shows antitumoral properties.

Liarozole (Standard) is the analytical standard of Liarozole. This product is intended for research and analytical applications. Liarozole (R75251; R85246) is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of retinoic acid (IC50=7 μM), resulting in increased tissue levels of retinoic acid. Liarozole shows antitumoral properties.