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Androgen Receptor

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).

Androgen Receptor Related Products (62):

Cat. No. Product Name Effect Purity
  • HY-70002
    Enzalutamide Antagonist 99.71%
    Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells. Enzalutamide is an autophagy activator[1][2].
  • HY-14650
    DHEA Inhibitor >98.0%
    DHEA (Prasterone) is one of the most abundant steroid hormones. DHEA (Prasterone) mediates its action via multiple signaling pathways involving specific membrane receptors and via transformation into androgen and estrogen derivatives (e.g., androgens, estrogens, 7α and 7β DHEA, and 7α and 7β epiandrosterone derivatives) acting through their specific receptors.
  • HY-16060
    Apalutamide Antagonist 99.97%
    Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM[1].
  • HY-16985
    Darolutamide Antagonist 99.03%
    Darolutamide (ODM-201;BAY-1841788) is a potent androgen receptor (AR) antagonist with an IC50 of 26 nM in in vitro assay.
  • HY-B0469
    Medroxyprogesterone acetate 99.82%
    Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors[1]
  • HY-130992
    Androgen receptor antagonist 1 Antagonist
    Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC50 of 59 nM[1]. Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively[2].
  • HY-130492
    ARCC-4 Inhibitor
    ARCC-4 is a low-nanomolar androgen receptor (AR) degrader based on PROTAC, with a DC50 of 5 nM. ARCC-4 is an enzalutamide-based von Hippel-Lindau (VHL)-recruiting AR PROTAC and outperforms enzalutamide. ARCC-4 effectively degrades clinically relevant AR mutants associated with antiandrogen therapy[1].
  • HY-111848
    PROTAC AR Degrader-4 Inhibitor
    PROTAC AR Degrader-4 comprises a cIAP1 ligand binding group, a linker and an androgen receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1].
  • HY-14249
    Bicalutamide Agonist 99.62%
    Bicalutamide is a non-steroidal androgen receptor inhibitor.
  • HY-B0022
    Flutamide Antagonist 99.77%
    Flutamide is an antiandrogen drug, with its active metablolite binding at androgen receptor with Ki values of 55 nM, and primarily used to treat prostate cancer.
  • HY-B1029
    Danazol Agonist 99.91%
    Danazol is a derivative of the synthetic steroid ethisterone, that suppresses the production of gonadotrophins, and has some weak androgenic effects.
  • HY-B0561
    Spironolactone Antagonist 99.05%
    Spironolactone is a potent antagonist of the androgen receptor.
  • HY-15194
    Dimethylcurcumin Inhibitor 98.19%
    Dimethylcurcumin (ASC-J9) is an androgen receptor degradation enhancer that effectively suppresses castration resistant prostate cancer cell proliferation and invasion.
  • HY-B1269
    Testosterone propionate Agonist 99.89%
    Testosterone propionate is a slower releasing anabolic steroid used mainly in the treatment of low testosterone levels in men.
  • HY-12111
    BMS-564929 Agonist 98.70%
    BMS-564929 is an androgen receptor (AR) agonist, binds to androgen receptor (AR) with a Ki of 2.11±0.16 nM.
  • HY-16079
    AZD3514 Inhibitor 98.77%
    AZD3514 is a potent and oral androgen receptor downregulator with Ki of 2.2 μM and has ability of reducing AR protein expression.
  • HY-14383
    RAD140 Inhibitor 99.53%
    RAD140 is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM).
  • HY-70002A
    N-desmethyl Enzalutamide Antagonist 99.70%
    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[1].
  • HY-114530
    LY2452473 Modulator 99.24%
    LY2452473 is an orally bioavailable, selective androgen receptor modulator (SARM).
  • HY-112895
    UT-155 Antagonist 99.39%
    UT-155 is a selective and potent androgen receptor (AR) antagonist, with a Ki of 267 nM for UT-155 binding to AR-LBD.