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-160680
    AR antagonist 6
    		Inhibitor
    AR antagonist 6 (compound 6i) is a diphenyl ether androgen receptor (AR) antagonist that binds AR at a concentration of 120 nM. AR antagonist 6 exhibits low toxicity and in vitro activity against the golden Syrian hamster ear model.
    AR antagonist 6
  • HY-152512
    RLA-4842
    		Activator
    RLA-4842 is an iron activator containing anti-androgen. RLA-4842 has anti-proliferative activity on metastatic castration-resistant prostate cancer (mCRPC) cell line.
    RLA-4842
  • HY-151220
    Androgen receptor-IN-4
    		Inhibitor
    Androgen receptor-IN-4 (Compound 206) is an androgen receptor inhibitor, and can be used for research of Kennedy's disease.
    Androgen receptor-IN-4
  • HY-143535
    HG122
    HG122 promotes androgen receptor (AR) degradation through the proteasome pathway inhibiting the castration-resistant prostate cancer.
    HG122
  • HY-142923
    AR antagonist 2
    		Antagonist
    AR antagonist 2 (compound 58) is a potent androgen receptor (AR) inhibitor with an IC50 of 0.95 μM. AR antagonist 2 has the potential for cancer research.
    AR antagonist 2
  • HY-169349
    Androgen receptor antagonist 12
    		Antagonist
    Androgen receptor antagonist 12 (Compound EF2) is an orally active Androgen receptor (AR) antagonist (IC50: 0.30 μM). Androgen receptor antagonist 12 inhibits transcriptional activity of variant AR mutants and and the proliferation of AR-positive PCa cell lines. Androgen receptor antagonist 12 blocks AR nuclear translocation. Androgen receptor antagonist 12 inhibits tumor growth in a C4-2B xenograft mouse model. Androgen receptor antagonist 12 can be used for prostate cancer (PCa) research.
    Androgen receptor antagonist 12
  • HY-137444
    Ludaterone
    Ludaterone is an antiandrogen agent, with potent antiandrogenic activity.
    Ludaterone
  • HY-162702
    AZ'3137
    		Degrader 99.90%
    AZ‘3137 (Compound 22) is an orally active PROTAC-type androgen receptor (AR) degrader, with a DC50 value of 22 nM. AZ'3137 can inhibit cell proliferation of LNCaP, with a GI50 value of 74 nM. AZ'3137 can inhibit AR signaling and tumor growth in prostate cancer mice (Red: AR antagonists; Blue: CRBN ligand (HY-A0003); Black: linker).
    AZ'3137
  • HY-116214R
    Cyprodinil (Standard)
    		Agonist
    Cyprodinil (Standard) (CGA-219417 (Standard)) is the analytical standard of Cyprodinil (HY-116214). This product is intended for research and analytical applications. 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 (Standard)
  • HY-16060S3
    Apalutamide-d7
    		Antagonist
    Apalutamide-d7 is deuterated labeled Apalutamide (HY-16060). Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM.
    Apalutamide-d<sub>7</sub>
  • HY-155543
    Anticancer agent 135
    		Antagonist
    Anticancer agent 135 (compound 26h) is a potent androgen receptor (AR) antagonist. Anticancer agent 135 can effectively block AR nuclear translocation and inhibit AR/AR-V7 heterodimerization, thereby inhibiting downstream gene transcription. Anticancer agent 135 displays potent robust efficacy in prostate cancer xenograft models.
    Anticancer agent 135
  • HY-Y0978S2
    Boc-Glycine-2-13C
    		Antagonist
    Boc-Glycine-2-13C is a 13C-labeled Linuron. Linuron is a phenylurea herbicide that is widely used to control the growth of grass and weeds in various agriculture crops and in orchards. Linuron is a photosystem II inhibitor. Linuron is also a competitive a
    Boc-Glycine-2-<sup>13</sup>C
  • HY-159639
    BAY-2925976
    		Inhibitor
    BAY-2925976
  • HY-123012A
    Lubabegron fumarate
    		Antagonist
    Lubabegron fumarate is a potent modulator of β-adrenergic receptor (β-AR). Lubabegron fumarate demonstrates antagonistic behavior at the β1 and β 2 receptor subtypes and agonistic behavior at the β 3 receptor subtype in cattle. Lubabegron fumarate reduces NH3 gas emissions from an animal or its waste. Lubabegron fumarate is available as an animal supplement.
    Lubabegron fumarate
  • HY-113289R
    Brassicasterol (Standard)
    		Inhibitor
    L-Ornithine (hydrochloride) (Standard) is the analytical standard of L-Ornithine (hydrochloride). This product is intended for research and analytical applications. L-Ornithine hydrochloride is a non-proteinogenic amino acid, is mainly used in urea cycle removing excess nitrogen in vivo. L-Ornithine hydrochloride shows nephroprotective.
    Brassicasterol (Standard)
  • HY-120703
    RU 58642
    		Inhibitor
    RU 58642 is an orally active non-steroidal antiandrogen, which displays a strong and selective affinity for androgen receptor.
    RU 58642
  • HY-N12124
    Monascuspiloin
    		Inhibitor
    Monascuspiloin (Monascinol) exhibits anti-androgenic activity with an IC50 of 7 μM. Monascuspiloin inhibits viability of PC-3 and LNCaP with IC50 of 45 and 47 μM. Monascuspiloin induces apoptosis in LNCaP through inhibition of Akt/mTOR signaling pathway, induces autophagy through activation AMPK signaling pathway and arrest cell cycle at G2/M phase in PC-3. Monascuspiloin exhibits antitumor efficacy in mice.
    Monascuspiloin
  • HY-167655
    KF-19418
    		Inhibitor
    KF-19418 is an anti-androgen antisense oligonucleotide (ASO) and a hair follicle stimulator. KF-19418 directly stimulated hair follicle in vitro and has hair growth promoting activities in vivo.
    KF-19418
  • HY-157455
    AR antagonist 5
    AR antagonist 5 (compound 30a) is a selective androgen receptor (AR) antagonist with an IC50 value of 134.8 nM. AR antagonist 5 has favorable pharmacokinetic properties and shows a high skin exposure and low plasma exposure[1.
    AR antagonist 5
  • HY-15758R
    3,3'-Diindolylmethane (Standard)
    		Antagonist
    3,3'-Diindolylmethane (Standard) is the analytical standard of 3,3'-Diindolylmethane. This product is intended for research and analytical applications. 3,3'-Diindolylmethane is a strong, pure androgen receptor (AR) antagonist.
    3,3'-Diindolylmethane (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity