2. Signaling Pathways
  3. Vitamin D Related/Nuclear Receptor
  4. Androgen Receptor

Androgen Receptor

Androgen Receptor

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Androgen receptor (AR) is a type of nuclear receptor that is activated by binding of either of the androgenic hormones testosterone or dihydrotestosterone in the cytoplasm and then translocating into the nucleus. Upon binding the hormone ligand, the receptor dissociates from accessory proteins, translocates into the nucleus, dimerizes, and then stimulates transcription of androgen responsive genes. The androgen receptor is most closely related to the progesterone receptor, and progestins in higher dosages can block the androgen receptor. The main function of the androgen receptor is as a DNA-binding transcription factor that regulates gene expression. Androgen regulated genes are critical for the development and maintenance of the male sexual phenotype. Mutations in this gene are also associated with complete androgen insensitivity (CAIS).

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-164477
    FL442
    		Modulator
    FL442 is an Androgen Receptor (AR) modulator. FL442 exhibits strong inhibitory effects in AR-dependent prostate cancer cells, showing similar inhibitory efficiency to traditional antiandrogen drugs Bicalutamide (HY-14249) and Enzalutamide (HY-70002), while maintaining antiandrogenic activity against the AR mutant F876L, which is highly resistant to Enzalutamide. Pharmacokinetic studies of FL442 in mice reveal a long half-life (8 hours), good targeting (prostate tissue), and metabolic stability, and it effectively inhibits LNCaP tumor growth at low plasma concentrations (30 ng/mL).
    FL442
  • HY-B1234S
    Octinoxate-13C,d3
    		Modulator
    Octinoxate-13C,d3 is the deuterium labeled Octinoxate (HY-W245806). Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to type II deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibits CYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo.
    Octinoxate-<sup>13</sup>C,d<sub>3</sub>
  • HY-15194R
    Dimethylcurcumin (Standard)
    		Inhibitor
    Dimethylcurcumin (Standard) is the analytical standard of Dimethylcurcumin. This product is intended for research and analytical applications. Dimethylcurcumin (ASC-J9) is an androgen receptor degradation enhancer that effectively suppresses castration resistant prostate cancer cell proliferation and invasion.
    Dimethylcurcumin (Standard)
  • HY-14249R
    Bicalutamide (Standard)
    		Antagonist
    Bicalutamide (Standard) is the analytical standard of Bicalutamide. This product is intended for research and analytical applications. Bicalutamide is an orally active non-steroidal androgen receptor (AR) antagonist. Bicalutamide can be used for the research of prostate cancer.
    Bicalutamide (Standard)
  • HY-13331S1
    Clascoterone-d6
    		Antagonist
    Clascoterone-d6 (Cortexolone 17 alpha-propionate-d6) is deuterium labeled Clascoterone. Clascoterone (Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate;CB-03-01) is a new topical and peripherally selective androgen antagonist.
    Clascoterone-d<sub>6</sub>
  • HY-114744
    6α-Hydroxy metandienone
    6α-Hydroxy metandienone is an androgenic anabolic steroid metabolite of Metandienone.
    6α-Hydroxy metandienone
  • HY-B1234A
    (E)-Octinoxate
    		Inhibitor
    (E)-Octinoxate is the isomer of Octinoxate (HY-B1234). Octinoxate is an organic compound that is an ingredient in some sunscreens and lip balms, primarily used is in sunscreens and other cosmetics to absorb UV-B rays from the sun, protecting the skin from damage and can be used to reduce the appearance of scars. Octinoxate also has a complex androgenic and estrogenic effect.
    (E)-Octinoxate
  • HY-131953
    Androgen receptor-IN-3
    		Inhibitor
    Androgen receptor-IN-3 (Compound 22) is an androgen receptor inhibitor. Androgen receptor-IN-3 inhibits AR-driven transcriptional activity in LNCaP cells, with an IC50 of 5.04 μM.
    Androgen receptor-IN-3
  • HY-13702R
    Nilutamide (Standard)
    		Antagonist
    Nilutamide (Standard) is the analytical standard of Nilutamide. This product is intended for research and analytical applications. Nilutamide (Nilandron) is an orally active nonsteroidal androgen receptor antagonist with affinity for androgen receptors but not for progestogen, estrogen or glucocorticoid receptors. Nilutamide can be used to research prostate cancer. Nilutamide also has antischistosomal properties.
    Nilutamide (Standard)
  • HY-13331R
    Clascoterone (Standard)
    		Antagonist
    Clascoterone (Standard) is the analytical standard of Clascoterone. This product is intended for research and analytical applications. Clascoterone (Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate;CB-03-01) is a new topical and peripherally selective androgen antagonist.
    Clascoterone (Standard)
  • HY-161701
    (3β,4β,17β)-17-(2-Pyridinylmethyl)androst-5-ene-3,4,17-triol
    (3β,4β,17β)-17-(2-Pyridinylmethyl)androst-5-ene-3,4,17-triol is an androstane derivative with anticancer activity.
    (3β,4β,17β)-17-(2-Pyridinylmethyl)androst-5-ene-3,4,17-triol
  • HY-70002AR
    N-desmethyl Enzalutamide (Standard)
    		Antagonist
    N-desmethyl Enzalutamide (Standard) is the analytical standard of N-desmethyl Enzalutamide. This product is intended for research and analytical applications. N-desmethyl Enzalutamide is the active metabolite of Enzalutamide.N-desmethyl Enzalutamide is the active metabolite of Enzalutamide. N-desmethyl Enzalutamide demonstrates primary and secondary pharmacodynamics of similar potency to Enzalutamide and circulates at approximately the same plasma concentrations as enzalutamide.
    N-desmethyl Enzalutamide (Standard)
  • HY-B0846R
    Dimethomorph (Standard)
    		Inhibitor
    Dimethomorph (Standard) is the analytical standard of Dimethomorph. This product is intended for research and analytical applications. Dimethomorph is a fungicide belongs to the fungicide group of sterol biosynthesis inhibitor. Dimethomorph can inhibit fungal cell wall formation. Dimethomorph also inhibits androgen receptor (AR) activity in MDA-kb2 cells with an IC20 of 0.263 µM.
    Dimethomorph (Standard)
  • HY-164371
    (+)-JJ-74-138
    		Antagonist
    (+)-JJ-74-138, a novel non-competitive androgen receptor (AR) antagonist, is capable of inhibiting Enzalutamide-resistant CRPC.
    (+)-JJ-74-138
  • HY-105122
    Zanoterone
    		Antagonist
    Zanoterone is an orally active antagonist of the androgen receptor (AR) with a Ki of 2.2 μM. Zanoterone blocks the binding of androgens such as testosterone and dihydrotestosterone (DHT), inhibiting the androgen signaling pathway, thereby reducing androgen-dependent prostate hyperplasia and prostate cancer growth.
    Zanoterone
  • HY-175457
    AR-DBD ligand-Linker Conjugate 1
    AR-DBD ligand-Linker Conjugate 1 is a conjugate of AR-DBD ligand and linker. AR-DBD ligand-Linker Conjugate 1 can be used to synthesize PROTAC LYA914 (HY-175455).
    AR-DBD ligand-Linker Conjugate 1
  • HY-138089
    17β-Hydroxy exemestane
    		Agonist
    17β-Hydroxy exemestane (17-H-EXE) is the primary active metabolite of Exemestane (HY-13632). 17β-Hydroxy exemestane is an aromatase inhibitor (IC50 = 69 nM) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). 17β-Hydroxy exemestane stimulates growth of AR- and ERα-positive MCF-7 (EC50= 2.7 μM) and T47D breast cancer cells (EC50s = 0.43 and 1500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7 cells. 17β-Hydroxy exemestane inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae in ovariectomized rats.
    17β-Hydroxy exemestane
  • HY-114913
    Fenarimol
    		Inhibitor
    Fenarimol (EL 222) is a potent and orally active fungicide. Fenarimol also is a androgen receptor inhibitor with an IC50 value of 19 µM. Fenarimol decreases the mRNA expression of PBP C3, ODC, IGF-1.
    Fenarimol
  • HY-B0845R
    Prochloraz (Standard)
    		Antagonist
    Prochloraz (Standard) is the analytical standard of Prochloraz. This product is intended for research and analytical applications. Prochloraz is an imidazole antifungal. Prochloraz is as an estrogen receptor (ER) and androgen receptor (AR) antagonist and an aromatase inhibitor with IC50 values of 25 μM, 4 μM and 0.3 μM, respectively. Prochloraz is able to activate the aryl hydrocarbon receptor (AhR) having an EC50 of 1 μM.
    Prochloraz (Standard)
  • HY-106104
    Inocoterone acetate
    Inocoterone acetate (RU-38882) is a nonsteroidal antiandrogen. Inocoterone acetate binds to the androgen receptor and has antiandrogenic activity in animal models. Inocoterone acetate reduces inflammatory papules and pustules.
    Inocoterone acetate
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity