RAR/RXR Inhibitor

RAR/RXR Inhibitors (20):

Cat. No.	Product Name	Effect	Purity

HY-108529

BMS493	Inhibitor	99.94%
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.

HY-106019A

Liarozole hydrochloride	Inhibitor
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.

HY-14531

Talarozole	Inhibitor	99.61%
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.

HY-15373

Fenretinide	Inhibitor	99.15%
Fenretinide (4-HPR) is a synthetic retinoid deriverative, binding to the retinoic acid receptors (RAR) at concentrations necessary to induce cell death.

HY-107500

UVI 3003	Inhibitor	99.72%
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.

HY-100008

Peretinoin	Inhibitor	99.79%
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.

HY-10291

Tarenflurbil	Inhibitor	99.96%
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.

HY-153122A

YCT529	Inhibitor	≥98.0%
YCT529 is a potent, selective and orally active RAR-α inhibitor.

HY-111844

PROTAC RAR Degrader-1	Inhibitor
PROTAC RAR Degrader-1 comprises a IAP ligand binding group, a linker and a RAR ligand binding group. PROTAC RAR Degrader-1 is an RAR degrader. Maximal RAR degradation at 30 μM concentration in HT1080 cells. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs).

HY-N10361

Drupanin	Inhibitor	98.05%
Drupanin is an orally active selective AKR1C3 enzyme inhibitor and an RXRα agonist with an EC₅₀ value of 4.8 μM, which is isolated from green propolis. Drupanin also activates PPARγ moderately. Drupanin induces adipogenesis and elevates aP2 mRNA levels in 3T3-L1 fibroblasts Drupanin has the potential for the research of breast and prostate cancers.

HY-116506

Bigelovin	Inhibitor	99.92%
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.

HY-106019

Liarozole	Inhibitor	98.83%
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.

HY-106019C

Liarozole dihydrochloride	Inhibitor	≥99.0%
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.

HY-14653

Amsilarotene	Inhibitor	99.70%
Amsilarotene (TAC-101; Am 555S), an orally active synthetic retinoid, has selective affinity for retinoic acid receptor α (RAR-α) binding with K_i of 2.4, 400 nM for RAR-α and RAR-β. Amsilarotene induces the apoptotic of human gastric cancer, hepatocellular carcinoma and ovarian carcinoma cells. Amsilarotene can be used for the research of cancer.

HY-14802D

(-)-Talarozole	Inhibitor	98.12%
(-)-Talarozole is a potent inhibitor of retinoic acid metabolism extracted from patent WO 1997049704 A1.

HY-133739

NBD-125	Inhibitor
NBD-125 (B-12), a berberine analogue, is an RXRα activator, with an IC₅₀ of 31.10 μM in KM12C cell.

HY-14802C

(+)-Talarozole	Inhibitor	99.28%
(+)-Talarozole is a potent inhibitor of retinoic acid metabolism extracted from patent WO 1997049704 A1.

HY-10291R

Tarenflurbil (Standard)	Inhibitor
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.

HY-117926

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

HY-153122

YCT529 free acid	Inhibitor
YCT529 free acid is a potent, selective and orally active RAR-α inhibitor.

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