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-18102A
    GLPG0492 (R enantiomer)
    Modulator 99.51%
    GLPG0492 R enantiomer is the R enantiomer of GLPG0492. GLPG0492 is an orally active, non-steroidal selective androgen receptor modulator.
    GLPG0492 (R enantiomer)
  • 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-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-159844
    Gridegalutamide
    Gridegalutamide has antiandrogen and antitumor activities.
    Gridegalutamide
  • 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-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-113233
    19-Noretiocholanolone
    99.9%
    19-Noretiocholanolone is an anabolic androgenic steroid metabolite of Nandrolone.
    19-Noretiocholanolone
  • HY-P10413
    SHBG(141–161)
    Agonist 98.78%
    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
    99%
    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-14250A
    (Rac)-PF-998425
    Antagonist 99.45%
    (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-141901S1
    DHEA-d5
    DHEA-d5 (Prasterone-d5; Dehydroisoandrosterone-d5; Dehydroepiandrosterone-d5) is the deuterium labeled DHEA (HY-14650). 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.
    DHEA-d<sub>5</sub>
  • HY-16060S
    Apalutamide-d4
    Antagonist 99.90%
    Apalutamide-d4 is a deuterium labeled Apalutamide. Apalutamide is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM.
    Apalutamide-d<sub>4</sub>
  • HY-176068
    3-Cl-Pyridine-amide-acrylaldehyde-piperazine
    99.30%
    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-16060S1
    Apalutamide-d3
    Apalutamide-d3 is the deuterium labeled Apalutamide. Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM.
    Apalutamide-d<sub>3</sub>
  • HY-B0561S1
    Spironolactone-d3
    Antagonist 99.87%
    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-144127
    AR antagonist 3
    Antagonist 99.96%
    AR antagonist 3 is a potent and selective androgen receptor (AR) antagonist with an IC50 of 0.47 µM. AR antagonist 3 exhibits a dose-dependent decrease of the FRET signal (IC50= 18.05 μM). AR antagonist 3 shows effective inhibition on tumor growth when administered intratumorally.
    AR antagonist 3
  • 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-N9917
    Galloylalbiflorin
    Antagonist
    Galloylalbiflorin (6′-O-Galloylalbiflorin) is an androgen receptor (AR) antagonist (IC50=53.3 μM) and can be found in the roots of Paeonia lactiflora. Galloylalbiflorin shows anti-androgens activity.
    Galloylalbiflorin
  • HY-179433
    PROTAC AR Degrader-12
    Degrader
    PROTAC AR Degrader-12 is a highly efficient PROTAC targeting AR coactivator binding site (AR-CBS). PROTAC AR Degrader-12 induces AR degradation in a ubiquitin proteasome system (UPS) pathway-dependent manner. PROTAC AR Degrader-12 inhibits tumor cell growth by affecting DNA replication and cell division PROTAC AR Degrader-12 could not only effectively degrade AR, but also potently inhibit the proliferation of MCF-7 and multiple mutant or resistant BC cells. PROTAC AR Degrader-12 effectively blocked estrogen receptor α (ERα) signaling through a dual mechanism involving ERα protein downregulation and suppression of its transcriptional activity. PROTAC AR Degrader-12 significantly inhibits the mRNA expression of FOXA1, GREB1, SRC, and PELP1. PROTAC AR Degrader-12 can be used for the study of breast cancer.
    PROTAC AR Degrader-12
  • HY-176521A
    AR/BRD4 RIPTAC-1 TFA
    Ligand 99.61%
    AR/BRD4 RIPTAC-1 (Compound II-5) TFA is an orally active Regulatory-inducible proximity-targeting chimera (RIPTAC). AR/BRD4 RIPTAC-1 TFA induces the formation of a stable ternary complex between the androgen receptor (AR) and BRD4, thereby blocking BRD4 function. AR/BRD4 RIPTAC-1 TFA inhibits the growth and proliferation of tumor cells. AR/BRD4 RIPTAC-1 TFA holds promise for use in prostate cancer research.
    AR/BRD4 RIPTAC-1 TFA
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity