RAR/RXR Inhibitor

Fenretinide (4-HPR) is a synthetic retinoid deriverative, binding to the retinoic acid receptors (RAR) at concentrations necessary to induce cell death.

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.

Peretinoin is an oral acyclic retinoid with a vitamin A-like structure that targets retinoid nuclear receptors such as retinoid X receptor (RXR) and retinoic acid receptor (RAR). Peretinoin reduces the mRNA level of sphingosine kinase 1 (SPHK1) in vitro by downregulating a transcription factor, Sp1. Peretinoin prevents the progression of non-alcoholic steatohepatitis (NASH) and the development of hepatocellular carcinoma (HCC) through activating the autophagy pathway by increased Atg16L1 expression. Peretinoin inhibits HCV RNA amplification and virus release by altering lipid metabolism with a EC₅₀ of 9 μM.

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.

Bigelovin, a sesquiterpene lactone isolated from Inula hupehensis, is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation.

(+)-Talarozole is a potent inhibitor of retinoic acid metabolism extracted from patent WO 1997049704 A1.

RXR antagonist 5 (compound 22) is a selective retinoic acid X receptor (RXR) antagonist with binding potential to RXR evaluated by modeling.

(-)-Talarozole is a potent inhibitor of retinoic acid metabolism extracted from patent WO 1997049704 A1.

Talarozole (Standard) is the analytical standard of Talarozole. This product is intended for research and analytical applications. Talarozole (R115866) is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA) which increases intracellular levels of endogenous all-trans retinoic acid (RA). Talarozole inhibits both CYP26A1 and CYP26B1 with IC50s of 5.4 and 0.46 nM, respectively.

Peretinoin (Standard) is the analytical standard of Peretinoin. This product is intended for research and analytical applications. Peretinoin is an oral acyclic retinoid with a vitamin A-like structure that targets retinoid nuclear receptors such as retinoid X receptor (RXR) and retinoic acid receptor (RAR). Peretinoin reduces the mRNA level of sphingosine kinase 1 (SPHK1) in vitro by downregulating a transcription factor, Sp1[1]. Peretinoin prevents the progression of non-alcoholic steatohepatitis (NASH) and the development of hepatocellular carcinoma (HCC) through activating the autophagy pathway by increased Atg16L1 expression[2]. Peretinoin inhibits HCV RNA amplification and virus release by altering lipid metabolism with a EC50 of 9 μM[3].

Liarozole hydrochloride is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole hydrochloride inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of retinoic acid (IC₅₀=7 μM), resulting in increased tissue levels of retinoic acid. Liarozole hydrochloride shows antitumoral properties.

ZSH-512 is a potent RARγ inhibitor. ZSH-512 shows antiproliferation activity. ZSH-512 induces apoptosis. ZSH-512 decreases CD133, NANOG, SOX2, and EPCAM protein expression. ZSH-512 shows anticancer activity. ZSH-512 has the potential for the research of colorectal cancer.

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.

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.

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.

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.