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-162423
    CYB210010
    Agonist
    CYB210010 is an orally bioavailable, long-acting serotonin 5-HT2 receptor agonist that selectively targets 5-HT2A and 5-HT2C receptors (EC50: 4.1 n, 7.3 nM). CYB210010 can enter the central nervous system, cause a head twitch response (HTR), and is not prone to behavioral tolerance during chronic administration.
    CYB210010
  • HY-14249S
    Bicalutamide-d4
    Antagonist
    Bicalutamide-d4 is the deuterium labeled Bicalutamide. Bicalutamide is an orally active non-steroidal androgen receptor (AR) antagonist. Bicalutamide can be used for the research of prostate cancer.
    Bicalutamide-d<sub>4</sub>
  • HY-403733B
    (+)-JJ-450
    Antagonist
    (+)-JJ-450 is a non-competitive antagonist targeting the androgen receptor (AR) that inhibits AR nuclear localization and transcriptional activity in the absence of androgen. (+)-JJ-450 is less active than (-)-JJ-450 (HY-403733A) in inhibiting prostate-specific antigen (PSA) expression in LN95 cells, possibly because (+)-JJ-450 targets the ligand binding domain (LBD) of AR. (+)-JJ-450 inhibits the transcriptional activity of AR and its splice variants (e.g., ARv7) by promoting the degradation of unliganded AR in the nucleus and reducing the binding of AR to androgen response elements (AREs). (+)-JJ-450 can be used in castration-resistant prostate cancer (CRPC) studies that are resistant to enzalutamide (MDV3100) (HY-70003).
    (+)-JJ-450
  • HY-113233
    19-Noretiocholanolone
    19-Noretiocholanolone is an anabolic androgenic steroid metabolite of Nandrolone.
    19-Noretiocholanolone
  • HY-173640
    ID11916
    Antagonist
    ID11916 is an orally active androgen receptor (AR) antagonist and a phosphodiesterase 5 (PDE5) inhibitor. ID11916 blocks androgen binding to AR, nuclear translocation, and androgen-dependent transcriptional activity of AR, while increasing intracellular cGMP levels and activating PKG via inhibition. ID11916 shows potent anti-cancer effect in prostate cancer cell lines VCaP and 22Rv1 and in AR-positive breast cancer cell lines SK-BR-3.
    ID11916
  • HY-135473
    Chlormadinone
    Inhibitor
    Chlormadinone is an antiandrogen agent. Chlormadinone can be used for the study of benign prostatic hyperplasia (BPH).
    Chlormadinone
  • HY-W411296
    6α-Chloro testosterone
    6α-Chloro testosterone is an anabolic androgenic steroid.
    6α-Chloro testosterone
  • HY-P10413
    SHBG(141–161)
    Agonist
    SHBG 141-161 is a GPRC6A receptor agonist. SHBG 141-161 mimics the action of GPRC6A endogenous agonist uncarboxylated osteocalcin by binding to GPRC6A and promoting downstream signaling to increase testosterone and insulin secretion. SHBG 141-161 also reduces the affinity of GPRC6A to GDP protein by binding to the outer cell domain of GPRC6A thus affecting the dynamics of signal transduction. SHBG 141-161 can be used to study GPRC6A in energy metabolism and endocrine regulation.
    SHBG(141–161)
  • HY-B1986S
    p,p'-DDE-d8
    p,p'-DDE-d8 is the deuterium labeled p,p'-DDE. p,p'-DDE (4,4'-DDE), a major metabolite of persistent dichlorodiphenyltrichloroethane (DDT), is a potent androgen receptor antagonist, with an IC50 of 5 μM and a Ki of 3.5 μM.
    p,p'-DDE-d<sub>8</sub>
  • HY-172954
    Androgen receptor ligand 1
    Androgen receptor ligand 1 is an androgen receptor (AR) ligand. Androgen receptor ligand 1 binds to CRBN E3 ligase via a linker to form an AR PROTAC degrader. Androgen receptor ligand 1 can be used in the study of prostate cancer.
    Androgen receptor ligand 1
  • HY-153276
    Androgen receptor-IN-5
    Inhibitor
    Androgen receptor-IN-5 is an androgen receptor inhibitor with potent anticancer effects. Androgen receptor-IN-5 also inhibits the production of IL-17A, IL- 17F and INF-γ (WO2023281097A1,Example 1/1).
    Androgen receptor-IN-5
  • HY-149914
    WCA-814
    Degrader
    WCA-814 is an androgen receptor (AR) antagonist-Hsp90 inhibitor conjugate. WCA-814 induces the degradation of full-length and AR-V7. WCA-814 has cytotoxic effect in prostatic cancer cells (IC50: 171.2 nM, 26.5 nM for LNCaP, 22Rv1 cell).
    WCA-814
  • HY-173372
    PROTAC AR Degrader-10
    Degrader
    PROTAC AR Degrader-10 is a protein degrader targeting the androgen receptor (AR) with a DC50 value ≤100 nM. PROTAC AR Degrader-10 can be used for prostate cancer study. (Structure Note: Pink: target protein ligand (HY-173373); Blue: E3 ligase ligand (HY-138793); Black: linker) .
    PROTAC AR Degrader-10
  • HY-149452
    SJ1008066
    Inhibitor
    SJ1008066 is a MAGE-A11 inhibitor with anIC50 of 0.13 μM. SJ 1008066 binds to the MAGE homology domain (MHD) and disrupts MAGE-A11:PCF11 interaction.
    SJ1008066
  • HY-116214S1
    Cyprodinil-13C6
    Agonist
    Cyprodinil-13C6 (CGA-219417-13C6) is the 13C6 labeled Cyprodinil (HY-116214). Cyprodinil (CGA-219417) is a broad-spectrum anilinopyrimidine fungicide and an activator of the aryl hydrocarbon receptor. Cyprodinil also has anti-androgenic and androgenic activities. Cyprodinil can inhibit the biosynthesis of methionine in plant-pathogenic fungi and protect fruits and vegetables from a variety of pathogens.
    Cyprodinil-<sup>13</sup>C<sub>6</sub>
  • HY-172612
    AR antagonist 13
    Antagonist
    AR antagonist 13 (compound 19) is an androgen receptor antagonist with inhibition rates exceeding 71.5% at 10 μM. AR antagonist 13 inhibits prostate cancer cell growth.
    AR antagonist 13
  • HY-152524
    Androgen receptor antagonist 7
    Antagonist
    Androgen receptor antagonist 7 is an effective androgen receptor (AR) antagonist with an IC50 value of 1.18 µM. Androgen receptor antagonist 7 has biological activity in vitro and inhibits the expression of AR target in a time and dose dependent manner with an GI50 value of 7.9 µM .
    Androgen receptor antagonist 7
  • HY-123163
    JNJ-1250132
    Inhibitor
    JNJ-1250132 (RWJ-66826) is an orally active and potent steroidal progesterone receptor (PR) antagonist, with an IC50 of 1.3 nM. JNJ-1250132 inhibits binding of the receptor to DNA in vitro. JNJ-1250132 is a potent competitive inhibitor of binding to the human glucocorticoid receptor (GR) (IC50=0.50 nM) and the rat androgen receptor (AR) (IC50=5.6 nM), and was a weak inhibitor of binding to human Estrogen receptor (ER) (IC50 >3000 nM).
    JNJ-1250132
  • HY-160659
    Androgen receptor antagonist 10
    Antagonist
    Androgen receptor antagonist 10 (compound 6h) is a androgen receptor antagonist. Androgen receptor antagonist 10 reduces the wax esters in the golden syrian hamster model.
    Androgen receptor antagonist 10
  • HY-122611
    CSRM617
    Inhibitor
    CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model
    CSRM617
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity