2. Signaling Pathways
  3. Vitamin D Related/Nuclear Receptor
  4. Androgen Receptor

Androgen Receptor

Androgen Receptor

Related Products

PDF 1.49 MB

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-19470
    Topilutamide
    		Inhibitor 99.91%
    Topilutamide is a topical nonsteroidal antiandrogen (NSAA).
    Topilutamide
  • HY-B0469R
    Medroxyprogesterone acetate (Standard)
    Medroxyprogesterone acetate (Standard) is the analytical standard of Medroxyprogesterone acetate. This product is intended for research and analytical applications. Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors.
    Medroxyprogesterone acetate (Standard)
  • HY-N6714
    Alternariol
    		Inhibitor 99.88%
    Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects.
    Alternariol
  • HY-19337
    Ketodarolutamide
    		Antagonist 98.72%
    Ketodarolutamide (ORM-15341) is a potent and full antagonist for human AR (hAR) with IC50 values of 38 nM as shown by transactivation assays in AR-HEK293 cells stably expressing full-length hAR and an androgen-responsive luciferase reporter gene construct.
    Ketodarolutamide
  • HY-W013272
    Hydroxyflutamide
    		Antagonist 99.77%
    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
  • HY-139436
    ARD-2585
    		Inhibitor 99.16%
    ARD-2585 is an exceptionally potent and orally active PROTAC degrader of androgen receptor.
    ARD-2585
  • HY-70002S1
    Enzalutamide-d6
    		Antagonist 99.85%
    Enzalutamide-d6 (MDV3100-d6) is a deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells.
    Enzalutamide-d<sub>6</sub>
  • HY-114530
    LY2452473
    		Modulator 99.93%
    LY2452473 is an orally bioavailable, selective androgen receptor modulator (SARM).
    LY2452473
  • HY-N6660
    Trisdecanoin
    		Inhibitor ≥98.0%
    Trisdecanoin (Tricaprin; Glyceryl tridecanoate) is an orally available precursor of decanoic acid (DA precursor) that can be hydrolyzed to decanoic acid. Trisdecanoin and its metabolite capric acid not only provide the body with a quick source of energy, but can also affect lipid metabolism. Trisdecanoin is a major component of medium chain triglycerides (MCT), which has preventive or inhibitory properties for abdominal aortic aneurysms (AAA), inhibition of cardiovascular disease, and anti-androgen (NSAA) and anti-hyperglycemic properties. Trisdecanoin can be used as an additive in food, medicine and cosmetics.
    Trisdecanoin
  • HY-107480
    YK11
    		Agonist 98.06%
    YK11 is a partial agonist of androgen receptor, with osteogenic activity.
    YK11
  • HY-114612
    11-Ketotestosterone
    		Agonist 99.90%
    11-Ketotestosterone (11-Oxotestosterone), an oxidized form of Testosterone, is an active androgen.
    11-Ketotestosterone
  • HY-123875A
    Ralaniten triacetate
    		Inhibitor 98.79%
    Ralaniten triacetate (EPI-506), the pro-agent of Ralaniten, is a first-in-class, orally active androgen receptor (AR) N-terminal domain (NTD) inhibitor. Ralaniten triacetate shows activity against both full length and resistance-related AR species, including AR-v7.
    Ralaniten triacetate
  • HY-B1405
    Dehydroisoandrosterone 3-acetate
    		Agonist ≥98.0%
    Dehydroepiandrosterone 3-acetate is a testosterone/estrogen precursor and known modulator of vertebrate aggression.
    Dehydroisoandrosterone 3-acetate
  • HY-N0475
    Triptophenolide
    		Antagonist 99.98%
    Triptophenolide is a colorless crystalline plate isolated from ethyl acetate extracts of Tripterygium wilfordii.
    Triptophenolide
  • HY-15194
    Dimethylcurcumin
    		Inhibitor 98.06%
    Dimethylcurcumin (ASC-J9) is an androgen receptor degradation enhancer that effectively suppresses castration resistant prostate cancer cell proliferation and invasion.
    Dimethylcurcumin
  • HY-114402
    ARD-69
    		Degrader 99.61%
    ARD-69 is a PROTAC degrader based on the E3 ubiquitin ligase VHL and targeting the androgen receptor, which can induce androgen receptor (AR) protein degradation in AR-positive prostate cancer cells. ARD-69 inhibits AR-regulated gene expression, binds to the AR ligand binding domain at one end and binds to VHL at the other end, prompting AR to be recruited to the E3 ubiquitin ligase complex, triggering proteasome degradation, thereby inhibiting AR signaling pathways and downstream gene expression (such as PSA, TMPRSS2). ARD-69 can be used to study the treatment of castration-resistant prostate cancer (mCRPC).
    ARD-69 is composed of a target protein ligand (pink part) AR antagonist 14 (HY-172624), a PROTAC linker (black part) tert-Butyl 4-ethynyl-[1,4'-bipiperidine]-1'-carboxylate (HY-W442074), and a VHL-type E3 ubiquitinase ligand (blue part) VH 101, acid (HY-47070); among them, the VHL ligand and the linker can form a conjugate VH 101-amide-piperidine-Pip-alkyne (HY-172625).
    ARD-69
  • HY-114165
    DJ-V-159
    		Agonist 99.94%
    DJ-V-159 is an agonist for G protein-coupled receptor family C group 6 member A (GPRC6A).
    DJ-V-159
  • HY-15103
    AH3960
    		Antagonist 99.92%
    AH3960 (compound 16c) is an antagonist of androgen receptor. AH3960 binds wild as well as T877 mutant type androgen receptors. AH3960 selectively inhibits T877 with an IC50 value of 0.82 μM. AH3960 also serves as an agonist of parathyroid hormone receptor-1 (PTHR1).
    AH3960
  • HY-110028
    Leelamine hydrochloride
    		Inhibitor 99.06%
    Leelamine hydrochloride is a tricyclic diterpene molecule that is extracted from the bark of pine trees. Leelamine hydrochloride is a cannabinoid receptor type 1 (CB1) agonist and a inhibitor of SREBP1-regulated fatty acid/lipid synthesis in prostate cancer cells that is not affected by androgen receptor status. Leelamine hydrochloride suppresses transcriptional activity of androgen receptor, which is known to regulate fatty acid synthesis[2,3].
    Leelamine hydrochloride
  • HY-11027
    MK-0773
    		Inhibitor 99.92%
    MK-0773 is a selective androgen receptor modulators (SARMs) that binds to AR with an IC50 of 6.6 nM.
    MK-0773
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity