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-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-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)
  • 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
  • HY-152850A
    Gumelutamide monosuccinate
    Antagonist
    Gumelutamide (monosuccinate) is a tetrahydropyridopyrimidine compound, acting as an antiandrogen, antineoplastic agent. Gumelutamide (monosuccinate) is an androgen antagonist.
    Gumelutamide monosuccinate
  • HY-122611R
    CSRM617 (Standard)
    Inhibitor
    CSRM617 (Standard) is the analytical standard of CSRM617. This product is intended for research and analytical applications. 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 (Standard)
  • HY-176068
    3-Cl-Pyridine-amide-acrylaldehyde-piperazine
    3-Cl-Pyridine-amide-acrylaldehyde-piperazine is a synthetic intermediate of LO-4-25 (HY-176067). LO-4-25 is an androgen receptor (AR) DNA binding domain ligand linked via a linker to the truncated fumaramide handle. LO-4-25 shows robust degradation of both AR and AR-V7 in 22Rv1 cells.
    3-Cl-Pyridine-amide-acrylaldehyde-piperazine
  • HY-14650R
    DHEA (Standard)
    Control
    DHEA (Prasterone) (Standard) is the analytical standard of DHEA. This product is intended for research and analytical applications. DHEA is a steroid hormone.
    DHEA (Standard)
  • HY-106827
    Trimegestone
    Inhibitor
    Trimegestone (RU 27987) is an orally active 19-norpregnane progestin. Trimegestone binds to progesterone receptor (PR) with an IC50 value of 3.3 nM (rat PR). Trimegestone increases alkaline phosphatase activity (EC50=0.1 nM) but not luciferase activity. Trimegestone also shows a weak antiandrogenic activity (weak androgen receptor affinity). Trimegestone can be used in studies of contraception or menopausal syndromes.
    Trimegestone
  • HY-P4779
    Acetyl-ACTH (2-24) (human, bovine, rat)
    Modulator
    Acetyl-ACTH (2-24) (human, bovine, rat) is a fragment of proopiomelanocortin (POMC) peptide. POMC peptides such as adrenocorticotrophin (ACTH), which is the precursor of α-MSH, is also an agonist at the MC-1 receptor.
    Acetyl-ACTH (2-24) (human, bovine, rat)
  • HY-156751
    (Rac)-GDC-2992
    Degrader
    (Rac)-GDC-2992 (Compound 1) is a PROTAC androgen receptor degrader (DC50: 10 nM in VCaP cell). (Rac)-GDC-2992 blocks the process of androgen receptor transduction and also degrades the receptor itself. (Rac)-GDC-2992 can be used for prostate cancer research. Pink: AR ligand (HY-130845); Blue: E3 ligase ligand (HY-W1003189); Black: linker (HY-169975).
    (Rac)-GDC-2992
  • HY-163813
    AR Degrader-2
    Degrader
    AR Degrader-2 (Compound 2) is a molecular glue that degrades androgen receptor (AR) with a DC50 of 0.3-0.5 μM in cell VCaP.
    AR Degrader-2
  • HY-157491
    K2-B4-5e
    Degrader
    K2-B4-5e is a E3 ligase KLHDC2-based BRD4 and androgen receptor (AR) degradation PROTAC. K2-B4-5e is capable of inducing rapid and robust degradation of BET-family and AR proteins in cells.
    K2-B4-5e
  • HY-W013272R
    Hydroxyflutamide (Standard)
    Antagonist
    Hydroxyflutamide (Standard) is the analytical standard of Hydroxyflutamide. This product is intended for research and analytical applications. Hydroxyflutamide (HF), an active metabolite of Flutamide, is a potent androgen receptor antagonist (IC50=700 nM). Hydroxyflutamide can be used for the research of prostate cancer.
    Hydroxyflutamide (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity