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

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).

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-164552
    ZNU-IMB-Z15
    Antagonist 98.07%
    ZNU-IMB-Z15 (Compound Z15) is an antagonist of the androgen receptor (AR) and also a selective degrader of AR and ARV7. ZNU-IMB-Z15 can directly bind to the ligand-binding domain (LBD) and activation function-1 region of AR, and promote AR degradation through the proteasome pathway. ZNU-IMB-Z15 effectively inhibits the transcriptional activity of AR, AR mutants, and AR splice variants (ARVs), downregulating the mRNA and protein levels of AR downstream target genes, thereby overcoming the resistance to second-generation antiandrogen drugs induced by AR LBD mutations, AR amplification, and ARVs in castration-resistant prostate cancer (CRPC). ZNU-IMB-Z15 can inhibit the proliferation of AR-positive CRPC cell lines and induce their apoptosis, demonstrating anticancer activity both in vivo and in vitro.
    ZNU-IMB-Z15
  • HY-135794S
    11-Ketodihydrotestosterone-d3
    Agonist ≥99.90%
    11-Ketodihydrotestosterone-d3 is the deuterium labeled 11-Ketodihydrotestosterone. 11-Ketodihydrotestosterone (11-KDHT; 5α-Dihydro-11-keto testosterone) is an endogenous steroid and a metabolite of 11β-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a potent androgen receptor (AR) agonist with a Ki of 20.4 nM and an EC50 of 1.35 nM for human AR. 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostate cancer cells.
    11-Ketodihydrotestosterone-d<sub>3</sub>
  • HY-B0469S
    Medroxyprogesterone acetate-d3
    98.13%
    Medroxyprogesterone acetate-d3 is deuterium labeled Medroxyprogesterone acetate. Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors.
    Medroxyprogesterone acetate-d<sub>3</sub>
  • HY-163340
    GA32
    Inhibitor 99.67%
    GA32 (compound 58r) is potent androgen receptor (AR)/glucocorticoid receptor (GR) dual inhibitor with IC50 values of 0.13 μM and 0.83 μM for AR and GR, respectively. GA32 inhibits the proliferation of Enzalutamide (HY-70002) resistance castration-resistant prostate cancer both in vitro and in vivo.
    GA32
  • HY-152844
    Faznolutamide
    Inhibitor 98.85%
    Faznolutamide is an antiandrogen agent.
    Faznolutamide
  • HY-103246
    TFM-4AS-1
    99.96%
    TFM-4AS-1 is a selective androgen receptor modulator (SARM), and a potent androgen receptor (AR) ligand with an IC50 of 38 nM. TFM-4AS-1 is a gene-selective agonist.
    TFM-4AS-1
  • HY-B0561S1
    Spironolactone-d3
    Antagonist 99.82%
    Spironolactone-d3 is the deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC50 of 24 nM. Spironolactone is also a potent antagonist of androgen receptor with an IC50 of 77 nM. Spironolactone promotes autophagy in podocytes.
    Spironolactone-d<sub>3</sub>
  • HY-B0561S
    Spironolactone-d7
    Antagonist 99.96%
    Spironolactone-d7 is the deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC50 of 24 nM. Spironolactone is also a potent antagonist of androgen receptor with an IC50 of 77 nM. Spironolactone promotes autophagy in podocytes.
    Spironolactone-d<sub>7</sub>
  • HY-112895A
    (R)-UT-155
    Inhibitor 98.09%
    (R)-UT-155 (compound 11) is a selective androgen receptor degrader (SARD) ligand. Less active than the S-isomer.
    (R)-UT-155
  • HY-N7045
    Isosilybin B
    Inhibitor 99.32%
    Isosilybin B is a flavonolignan. Isosilybin B can be isolated from Silybum marianum. Isosilybin B can regulate cell cycle-related proteins (e.g., reduce cyclins (D3, D1, A, E), Cdk4, Cdk2, Cdc25A), and activate Caspases (Caspase-9 and Caspase-3). Isosilybin B can promote Apoptosis, reduce androgen receptor (AR) and PSA. Isosilybin B has anticancer activity against prostate cancer.
    Isosilybin B
  • HY-112689
    Androgen receptor antagonist 9
    99.91%
    Androgen receptor antagonist 9 (compound 28) is an antagonist of the androgen receptor.
    Androgen receptor antagonist 9
  • HY-70002S
    Deutenzalutamide-d3
    Antagonist 99.81%
    Deutenzalutamide (Enzalutamide-d3) is a developed deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells.
    Deutenzalutamide-d<sub>3</sub>
  • HY-105318
    LGD-2226
    Modulator 98.58%
    LGD-2226 is a selective and orally active androgen receptor modulator with an EC50 of 0.2 nM and a Ki of 1.5 nM for human androgen receptor. LGD-2226 shows tissue selectivity in animal models, with reduced effects on prostate compared to muscle. LGD-2226 can be used for muscle wasting, osteoporosis and sexual dysfunction.
    LGD-2226
  • HY-W653723
    N-Nitrosodicyclohexylamine
    Antagonist ≥99.0%
    N-Nitrosodicyclohexylamine (NDCHA) is a N-nitrosocompound with anti-androgenic activities. N-Nitrosodicyclohexylamine shows the competitive binding to androgen receptor (AR) against 5α-dihydrotestosterone and decreased the level of AR protein.
    N-Nitrosodicyclohexylamine
  • HY-18102A
    GLPG0492 (R enantiomer)
    Modulator 99.51%
    GLPG0492 R enantiomer is the R enantiomer of GLPG-0492, which is a novel selective androgen receptor modulator.
    GLPG0492 (R enantiomer)
  • HY-W041703
    6-Amino-5-bromoquinoxaline
    Antagonist
    6-Amino-5-bromoquinoxaline is a 2-(arylamino)imidazole derivative and a precursor of α1- and α2-androgen receptor antagonists.
    6-Amino-5-bromoquinoxaline
  • HY-111848A
    PROTAC AR Degrader-4 TFA
    Inhibitor 99.26%
    PROTAC AR Degrader-4 comprises a IAP 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).
    PROTAC AR Degrader-4 TFA
  • HY-111848
    PROTAC AR Degrader-4
    Inhibitor
    PROTAC AR Degrader-4 comprises a IAP 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).
    PROTAC AR Degrader-4
  • HY-14250A
    (Rac)-PF-998425
    Antagonist 99.68%
    (Rac)-PF-998425 is a potent, selective, nonsteroidal androgen receptor (AR) antagonist. (Rac)-PF-998425 has IC50 values of 26 and 90 nM in the AR binding and cellular assays, respectively. (Rac)-PF-998425 has the potential for the research of the androgenetic alopecia.
    (Rac)-PF-998425
  • HY-70002R
    Enzalutamide (Standard)
    Antagonist
    Enzalutamide (Standard) is the analytical standard of Enzalutamide. This product is intended for research and analytical applications. Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells. Enzalutamide is an autophagy activator.
    Enzalutamide (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity