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-175455
    LYA914
    		Degrader
    LYA914 is an orally active AR/AR-V7 PROTAC degrader. LYA914 targets the proteolytic degradation of the conserved DNA binding domain (DBD) of the androgen receptor (AR). LYA914 exhibits potent antiproliferative effects in Enzalutamide (HY-70002)-insensitive/resistant cells. LYA914 inhibits tumor growth in VCaP/LNCaP tumor mouse models. LYA914 can be used to study castration-resistant prostate cancer (CRPC). (Pink: AR-DBD ligand-1: HY-175456, Blue: Thalidomide: HY-14658, Pink + Black: AR-DBD ligand-Linker Conjugate 1: HY-175457, Black: Boc-piperidine-oxopiperidin: HY-175458).
    LYA914
  • HY-146027
    Androgen receptor antagonist 4
    		Antagonist
    Androgen receptor antagonist 4 (Compound AT2) is an androgen receptor (AR) antagonist with an IC50 of 0.15 μM. Androgen receptor antagonist 4 efficiently antagonizes AR transcriptional activity, suppresses downstream target gene of AR, and blocks the DHT-induced AR nuclear translocation. Androgen receptor antagonist 4 shows anticancer activities.
    Androgen receptor antagonist 4
  • HY-111044
    (+)-JNJ-37654032
    		Modulator
    (+)-JNJ-37654032 is an orally active and selective androgen receptor modulator. (+)-JNJ-37654032 can be used in the study of muscle-wasting diseases.
    (+)-JNJ-37654032
  • 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-W713284
    2-Ethylhexyl (E)-3-(4-(methoxy-d3)phenyl)acrylate
    2-Ethylhexyl (E)-3-(4-(methoxy-d3)phenyl)acrylate is the deuterium labeled Octinoxate (HY-B1234). Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to type II deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibits CYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo.
    2-Ethylhexyl (E)-3-(4-(methoxy-d<sub>3</sub>)phenyl)acrylate
  • HY-W759219
    Adrenosterone-13C3
    Adrenosterone-13C3 ((+)-Adrenosterone-13C3) is the 13C-labeled Adrenosterone (HY-17462). 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-<sup>13</sup>C<sub>3</sub>
  • HY-162702
    AZ'3137
    		Degrader 99.90%
    AZ‘3137 is an orally active PROTAC-type androgen receptor (AR) degrader with a DC50 value of 22 nM. AZ‘3137 can degrade L702H mutant AR (DC50 of 92 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 (Pink: AR Ligand (HY-172954); Blue: CRBN ligand (HY-172955); Black: linker (HY-W262798); E3 Ligand+Linker: HY-172956).
    AZ'3137
  • 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-175652
    PROTAC Androgen receptor degrader-1
    		Degrader
    PROTAC Androgen receptor degrader-1 (Ex.14) is a PROTAC degrader targeting the androgen receptor with a DC50 of 6 nM. PROTAC Androgen receptor degrader-1 is used in prostate cancer research. (Structure Note: Pink: target protein ligand (HY-175654); Blue: E3 ligase ligand (HY-175654); Black: linker).
    PROTAC Androgen receptor degrader-1
  • HY-W744741
    Lupeol-d3
    Lupeol-d3 is the deuterium labeled Lupeol (HY-N0790). Lupeol is an active pentacyclic triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent?androgen receptor?(AR)?inhibitor and can be used for?cancer?research, especially prostate?cancer?of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC).
    Lupeol-d<sub>3</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 Boc-Glycine (HY-Y0978). Boc-Glycine is a Glycine (HY-Y0966) derivative.
    Boc-Glycine-2-<sup>13</sup>C
  • 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)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity