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-173373
    AR ligand-39
    		Antagonist
    AR ligand-39, an orally active and selective androgen receptor (AR) antagonist, is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). AR ligand-39 can be used for synthesis PROTAC AR Degrader-10 (HY-173372).
    AR ligand-39
  • HY-403733C
    JJ-450
    		Antagonist
    JJ-450 is a non-competitive antagonist androgen receptor (AR) that inhibits the transcriptional activity of wild-type AR and mutant ARF876L. JJ-450 has an IC50 of approximately 1-10 μM in inhibiting AR transcriptional activity in PC3 cells. It is selective for AR binding and does not compete with androgens for binding to the ligand binding domain (LBD) of AR. JJ-450 inhibits the transcriptional activity of AR and its splice variants (such as ARF876L) by inhibiting AR nuclear translocation and promoting the degradation of unliganded AR in the nucleus. JJ-450 can be used in castration-resistant prostate cancer (CRPC) studies that are resistant to Enzalutamide (MDV3100) (HY-70003).
    JJ-450
  • HY-P4786
    Acetyl-ACTH (7-24) (human, bovine, rat)
    Acetyl-ACTH (7-24) (human, bovine, rat) causes a marked decrease of ACTH-evoked corticosterone and aldosterone release.
    Acetyl-ACTH (7-24) (human, bovine, rat)
  • HY-W766769
    Cyproterone Acetate-13C2,d3
    		Antagonist
    Cyproterone Acetate-13C2,d3 is 13C-labeled Cyproterone Acetate (HY-13604).
    Cyproterone Acetate-<sup>13</sup>C<sub>2</sub>,d<sub>3</sub>
  • HY-153772
    Androgen receptor antagonist 8
    		Antagonist
    Androgen receptor antagonist 8 (Example 13) is an androgen receptor antagonist. Androgen receptor antagonist 8 inhibits prostate specific antigen secretion in LNcap cell (IC50: 88 nM). Androgen receptor antagonist 8 can be used for prostate cancer research.
    Androgen receptor antagonist 8
  • HY-173474
    ERβ agonist-1
    		Antagonist
    ERβ agonist-1 (Compound 8) is a dual-active selective ERβ agonist (EC50: 46.8 nM) and AR antagonist (IC50: 1555 nM). ERβ agonist-1 activates ERβ signaling by binding to ERβ and inhibits AR activity. ERβ agonist-1 retains selective ERβ agonist activity in mouse models and can be used to study prostate cancer.
    ERβ agonist-1
  • HY-17462R
    Adrenosterone (Standard)
    Adrenosterone (Standard) is the analytical standard of Adrenosterone. This product is intended for research and analytical applications. Adrenosterone ((+)-Adrenosterone) is a competitive hydroxysteroid (11-beta) dehydrogenase 1 (HSD11β1) inhibitor. Adrenosterone is a steroid hormone with weak androgenic effect. Adrenosterone is a dietary supplement that can decrease fat and increase muscle mass. Adrenosterone acts as a suppressor of metastatic progression of human cancer cells.
    Adrenosterone (Standard)
  • HY-173409
    AR antagonist 11
    		Antagonist
    AR antagonist 11 (Compound c2) is a selective AR antagonist with an IC50 of 0.019 μM. AR antagonist 11 is also effective against ARF877L/T878A mutant (IC50: 1.03 μM). AR antagonist 11 inhibits LNCaP cell proliferation and reduces PSA protein expression (IC50: 0.54 μM). AR antagonist 11 can be used for research of prostate cancer (PCa).
    AR antagonist 11
  • HY-162764
    Androgen receptor degrader-5
    		Degrader
    Androgen receptor degrader-5 (compound 14k) exhibits promising properties, including superior androgen receptor degradation activity and antiproliferative activity.
    Androgen receptor degrader-5
  • HY-171048
    GTx-027
    		Modulator 99.61%
    GTx-027 is an orally active and non-steroidal selective androgen receptor modulator (SARM). GTx-027 shows androgen receptor (AR) transactivation effects with the EC50 of 1.8 nM. GTx-027 acts selectively increase muscle weight (anabolic) without affecting secondary sexual organs (androgenic). GTx-027 has the protential for the study of breast cancer and stress urinary incontinence (SUI).
    GTx-027
  • HY-176521
    Antiproliferative agent-71
    		Inhibitor
    Antiproliferative agent-71 (Compound II-5) is an orally active dual inhibitor against the androgen receptor (AR) and bromodomain-containing protein 4 (BRD4). Antiproliferative agent-71 effectively inhibits tumor cell growth and proliferation by simultaneously blocking the functions of AR and BRD4. Antiproliferative agent-71 is promising for research of prostate cancer.
    Antiproliferative agent-71
  • HY-146026
    Androgen receptor antagonist 3
    		Antagonist
    Androgen receptor antagonist 3 (Compound C18) is an androgen receptor (AR) antagonist with an IC50 of 2.4 μM. Androgen receptor antagonist 3 shows anticancer activities.
    Androgen receptor antagonist 3
  • HY-139970
    VPC-13789
    		Inhibitor
    VPC-13789 is a potent, selective, and orally bioavailable antiandrogen. VPC-13789 can be used for the research of castration-resistant prostate cancer (CRPC) therapeutics. VPC-13789 inhibits androgen receptor (AR) transcriptional activity in LNCaP cells (IC50=0.19 μM).
    VPC-13789
  • HY-168299
    AR ligand-30
    		Ligand
    AR ligand-30 is a target protein ligand for PROTAC Bavdegalutamide (HY-138641), which can be used in prostate cancer research.
    AR ligand-30
  • HY-176067
    LO-4-25
    		Degrader
    LO-4-25 is a covalent degrader targeting the androgen receptor (AR) and its truncated variant AR-V7. LO-4-25 covalently binds to the E3 ubiquitin ligase CUL4 DCAF16, promoting the ubiquitination of AR and AR-V7, which subsequently are recognized and degraded by the proteasome, reducing the protein levels of AR and AR-V7 in cells. LO-4-25 is promising for research of androgen-independent prostate cancers.
    LO-4-25
  • HY-175456
    AR-DBD ligand-1
    AR-DBD ligand-1 is an AR-DBD ligand. AR-DBD ligand-1 can be used to synthesize PROTAC LYA914 (HY-175455).
    AR-DBD ligand-1
  • HY-N15686
    Torulene
    		Inhibitor
    Torulene (Torulin) is an orally active carotenoid with anti-cancer activity. Torulene inhibits proliferation and induces apoptosis of tumor cells via a mitochondrial signal pathway and the down-regulation of androgen receptor (AR) expression. Torulene can be used for the study of prostate cancer.
    Torulene
  • HY-100348R
    EPI-001 (Standard)
    		Inhibitor
    EPI-001 (Standard) is the analytical standard of EPI-001. This product is intended for research and analytical applications. EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer.
    EPI-001 (Standard)
  • HY-160547
    PROTAC AR Degrader-5
    		Inhibitor
    PROTAC AR Degrader-5 (compound A46) is a potent AR PROTACs degrader with an IC50 value of 49 nM. PROTAC AR Degrader-5 inhibits sebaceous plaque and induces hair regeneration (Pink: ligand for target protein (HY-169967); black: linker (HY-169966); Blue: E3 ligase ligand (HY-125845)).
    PROTAC AR Degrader-5
  • HY-103577
    LG-121071
    		Modulator
    LG-121071 is an orally active and selective androgen receptor modulator with a Ki of 17 nM.
    LG-121071
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity