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-135732
    SK33
    		Antagonist 99.98%
    SK33, a trifluoromethylated enobosarm analog, is a potent, and tissue selective anti-androgen. SK33reduces androgen receptor (AR) transcriptional activity.
    SK33
  • HY-164807
    SARD279
    		Degrader
    SARD279 is a potent and selective Androgen Receptor degrader with DC50 value of 1099 nM. SARD279 can be used in prostate cancer research.(Structure Note: Pink: target protein ligand (HY-117486); Blue,: Hyt (HY-W001578); Black: linker (HY-W004896))
    SARD279
  • HY-B1986
    p,p'-DDE
    		Antagonist 99.91%
    p,p'-DDE (4,4'-DDE) is the major and persistent metabolite of DDT. p,p'-DDE is a orally active androgen receptor antagonist with an IC50 of 5 μM and a Ki of 3.5 μM. p,p'-DDE can affect the development and function of the male reproductive system. Additionally, high serum concentrations of p,p'-DDE may be a risk factor for type 2 diabetes in women.
    p,p'-DDE
  • HY-161741
    VinclozolinM2-2204
    		Degrader 98.00%
    VinclozolinM2-2204 is a androgen receptor (AR) AUTOTAC degrader, with an DC50 of 200 nM in LNCaP prostate cancer cells. VinclozolinM2-2204 induces the formation of AR+LC3+ autophagic membranes. VinclozolinM2-2204 can be used for the research of cancer.(Pink: AR inhibitor (HY-168296); Black: linker (HY-128833); Blue: CRBN Ligand (HY-168293))
    VinclozolinM2-2204
  • HY-130845A
    AR antagonist 1 hydrochloride
    		Antagonist 99.53%
    AR antagonist 1 (compound 29) hydrochloride is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020).
    AR antagonist 1 hydrochloride
  • HY-139659
    ARD-61
    		Inhibitor 99.68%
    ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice. ARD-61 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    ARD-61
  • 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-16985S
    Darolutamide-d4
    		Antagonist 98.58%
    Darolutamide-d4 (ODM-201-d4) is deuterium labeled Darolutamide. Darolutamide (ODM-201;BAY-1841788) is a potent androgen receptor (AR) antagonist with an IC50 of 26 nM in in vitro assay.
    Darolutamide-d<sub>4</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-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-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 99.85%
    6-Amino-5-bromoquinoxaline is a 2-(arylamino)imidazole derivative and a precursor of α1- and α2-androgen receptor antagonists.
    6-Amino-5-bromoquinoxaline
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity