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-107480
    YK11
    		Agonist 98.06%
    YK11 is a partial agonist of androgen receptor, with osteogenic activity.
    YK11
  • 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-139436
    ARD-2585
    		Inhibitor 99.16%
    ARD-2585 is an exceptionally potent and orally active PROTAC degrader of androgen receptor.
    ARD-2585
  • HY-114530
    LY2452473
    		Modulator 99.93%
    LY2452473 is an orally bioavailable, selective androgen receptor modulator (SARM).
    LY2452473
  • HY-135331
    N-Desmethyl-Apalutamide
    		Antagonist 99.68%
    N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration.
    N-Desmethyl-Apalutamide
  • 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-19470
    Topilutamide
    		Inhibitor 99.91%
    Topilutamide is a topical nonsteroidal antiandrogen (NSAA).
    Topilutamide
  • HY-B0469R
    Medroxyprogesterone acetate (Standard)
    		99.24%
    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-19319
    MI-136
    		Inhibitor 99.04%
    MI-136 is an inhibitor of the menin-MLL protein-protein interaction (PPI), with an IC50 of 31 nM and a Kd of 23.6 nM. MI-136 shows to block AR signaling and has the potential for the study in castration-resistant tumors.
    MI-136
  • 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-114402
    ARD-69
    		Antagonist 99.75%
    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
  • 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-15996
    Seviteronel
    		Antagonist 99.83%
    Seviteronel (VT-464) is a potent CYP17 lyase inhibitor(h-Lyase IC50=69 nM) and an AR antagonist. Seviteronel demonstrates both exceptional in vitro lyase/hydroxylase selectivity (~10-fold) and oral activity in a hamster model of androgen biosynthesis inhibition.
    Seviteronel
  • 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-130992
    Androgen receptor antagonist 1
    		Antagonist 99.71%
    Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC50 of 59 nM. Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.
    Androgen receptor antagonist 1
  • HY-114612
    11-Ketotestosterone
    		Agonist 99.90%
    11-Ketotestosterone (11-Oxotestosterone), an oxidized form of Testosterone, is an active androgen.
    11-Ketotestosterone
  • HY-122025
    AC-262536
    		Agonist 99.94%
    AC-262536 is a selective and non-steroidal androgen receptor modulators (SARMs) with beneficial anabolic effects. AC-262536 exhibits potent agonist activity at the androgen receptor, with an affinity in the low nanomolar range (1-10 nM).
    AC-262536
  • HY-111024
    2,2,5,7,8-Pentamethyl-6-Chromanol
    		Modulator 99.30%
    2,2,5,7,8-Pentamethyl-6-Chromanol (PMC) is the anti-oxidant moiety of vitamin E (α-tocopherol). 2,2,5,7,8-Pentamethyl-6-Chromanol has potent androgen receptor (AR) signaling modulation and anti-cancer activity against prostate cancer cell lines.
    2,2,5,7,8-Pentamethyl-6-Chromanol
  • 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 99.96%
    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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity