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-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-145709
    Ar-V7-IN-1
    		Inhibitor 98.02%
    Ar-V7-IN-1 is a potent inhibitor of Ar-V7. AR-V7 is a hormone-independent splice variant of the androgen receptor. Ar-V7-IN-1 has the potential for the research of various indications, in particular cancers such as prostate cancer (extracted from patent WO2018114781A1, compound 43).
    Ar-V7-IN-1
  • HY-139436
    ARD-2585
    		Inhibitor 99.16%
    ARD-2585 is an exceptionally potent and orally active PROTAC degrader of androgen receptor.
    ARD-2585
  • 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-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-112895
    UT-155
    		Antagonist 99.55%
    UT-155 is a selective and potent androgen receptor (AR) antagonist, with a Ki of 267 nM for UT-155 binding to AR-LBD.
    UT-155
  • HY-112257
    S-23
    		Modulator 99.93%
    S-23 is an orally active selective androgen receptor modulator (SARM) with a Ki of 1.7 nM. S-23 induces androgen receptor (AR)-mediated transcriptional activation in CV-1 cells. S-23 increases prostate, seminal vesicle, and levator ani muscle weights in castrated rats.
    S-23
  • 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-115282A
    JNJ-63576253
    		Antagonist 99.22%
    JNJ-63576253 (TRC-253) is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 can be used for the research of castration-resistant prostate cancer (CRPC).
    JNJ-63576253
  • 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-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-N0475
    Triptophenolide
    		Antagonist 99.98%
    Triptophenolide is a colorless crystalline plate isolated from ethyl acetate extracts of Tripterygium wilfordii.
    Triptophenolide
  • 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 (HFT) is the active metabolite of Flutamide (HY-B0022) and exhibits oral activity. Hydroxyflutamide is a potent androgen receptor antagonist with an IC50 of 700 nM. Hydroxyflutamide can affect embryonic development and reproductive tract development in mice. Additionally, Hydroxyflutamide can enhance the efficacy of Bacillus Calmette-Guérin (BCG) to better inhibit the progression of bladder cancer. Hydroxyflutamide can be used in research related to tumors and reproductive diseases.
    Hydroxyflutamide
  • HY-152850
    Gumelutamide
    		Antagonist 99.00%
    Gumelutamide is a tetrahydropyridopyrimidine compound, acting as an antiandrogen, antineoplastic agent. Gumelutamide is an androgen antagonist.
    Gumelutamide
  • HY-B0561R
    Spironolactone (Standard)
    		Antagonist
    Spironolactone (Standard) is the analytical standard of Spironolactone. This product is intended for research and analytical applications. 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 (Standard)
  • 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-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>
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity