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-149452
    SJ1008066
    		Inhibitor
    SJ1008066 is a MAGE-A11 inhibitor with anIC50 of 0.13 μM. SJ 1008066 binds to the MAGE homology domain (MHD) and disrupts MAGE-A11:PCF11 interaction.
    SJ1008066
  • HY-P11660
    β-catenin-IN-10
    		Inhibitor
    β-catenin-IN-10 is a β-catenin:TCF4 interaction inhibitor with an IC50 of 5.44 μM. β-catenin-IN-10 inhibits the Wnt and AR signaling pathways with IC50 values of 0.105 μM and 1.02 μM, respectively. β-catenin-IN-10 suppresses the proliferation of castration-resistant prostate cancer cells. β-catenin-IN-10 is applicable to research related to prostate cancer.
    β-catenin-IN-10
  • HY-13604S1
    Cyproterone acetate-d6
    		Antagonist
    Cyproterone acetate-d6 is the deuterium labeled Cyproterone acetate (HY-13604). Cyproterone acetate is an anti-androgen (IC50=7.1 nM) and progestogen synthetic steroid. Cyproterone acetate has affinity with progesteron and with glucocorticoidal receptors.
    Cyproterone acetate-d<sub>6</sub>
  • HY-116214S1
    Cyprodinil-13C6
    		Agonist
    Cyprodinil-13C6 (CGA-219417-13C6) is the 13C6 labeled Cyprodinil (HY-116214). 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-<sup>13</sup>C<sub>6</sub>
  • HY-172612
    AR antagonist 13
    		Antagonist
    AR antagonist 13 (compound 19) is an androgen receptor antagonist with inhibition rates exceeding 71.5% at 10 μM. AR antagonist 13 inhibits prostate cancer cell growth.
    AR antagonist 13
  • HY-152524
    Androgen receptor antagonist 7
    		Antagonist
    Androgen receptor antagonist 7 is an effective androgen receptor (AR) antagonist with an IC50 value of 1.18 µM. Androgen receptor antagonist 7 has biological activity in vitro and inhibits the expression of AR target in a time and dose dependent manner with an GI50 value of 7.9 µM .
    Androgen receptor antagonist 7
  • HY-106614
    Osaterone acetate
    		Antagonist
    Osaterone acetate is an orally active steroid anti-androgen agent, mainly used for benign prostatic hyperplasia (BPH) in dogs. Osaterone acetate competitively antagonizes androgen receptor and inhibits 5α-reductase, reducing the concentration of dihydrotestosterone (DHT) while blocking the growth-stimulating effects of testosterone and DHT on prostate cells. Osaterone acetate can rapidly alleviate the symptoms of BPH in dogs without affecting the fertility of breeding dogs.
    Osaterone acetate
  • HY-123163
    JNJ-1250132
    		Inhibitor
    JNJ-1250132 (RWJ-66826) is an orally active and potent steroidal progesterone receptor (PR) antagonist, with an IC50 of 1.3 nM. JNJ-1250132 inhibits binding of the receptor to DNA in vitro. JNJ-1250132 is a potent competitive inhibitor of binding to the human glucocorticoid receptor (GR) (IC50=0.50 nM) and the rat androgen receptor (AR) (IC50=5.6 nM), and was a weak inhibitor of binding to human Estrogen receptor (ER) (IC50 >3000 nM).
    JNJ-1250132
  • HY-160659
    Androgen receptor antagonist 10
    		Antagonist
    Androgen receptor antagonist 10 (compound 6h) is a androgen receptor antagonist. Androgen receptor antagonist 10 reduces the wax esters in the golden syrian hamster model.
    Androgen receptor antagonist 10
  • HY-116267
    MHY219
    MHY219 is a histone deacetylase (HDAC) inhibitor with an IC50 of 0.276 μM. MHY219 inhibits total HDAC enzyme activity, increases histone H3 and H4 hyperacetylation. MHY219 induces cance cells phase arrest, apoptosis and inhibits proliferationin. MHY219 increases cleavage of PARP, Bax, cytochrome c levels, androgen receptor expression and decreases Bcl-2 expression. MHY219 can be used for the research of prostate cancer.
    MHY219
  • HY-122611
    CSRM617
    		Inhibitor
    CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model
    CSRM617
  • HY-152850A
    Gumelutamide monosuccinate
    		Antagonist
    Gumelutamide (monosuccinate) is a tetrahydropyridopyrimidine compound, acting as an antiandrogen, antineoplastic agent. Gumelutamide (monosuccinate) is an androgen antagonist.
    Gumelutamide monosuccinate
  • HY-B0333S
    Sulfamethizole-d4
    		Antagonist
    Sulfamethizole-d4 is the deuterium labeled Sulfamethizole (HY-B0333). Sulfamethizole is a sulfathiazole antibiotic. Sulfamethizole inhibits the synthesis of folic acid and thymine, and selectively suppresses Photobacterium phosphoreum bioluminescence. Sulfamethizole exerts antibacterial activity against Escherichia coli-mediated urinary tract infections but no activity against sulII gene-positive Escherichia coli. Sulfamethizole is applicable for the research of urinary tract infections and Photobacterium phosphoreum bioluminescence mechanisms.
    Sulfamethizole-d<sub>4</sub>
  • HY-122611R
    CSRM617 (Standard)
    		Inhibitor
    CSRM617 (Standard) is the analytical standard of CSRM617. This product is intended for research and analytical applications. CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model
    CSRM617 (Standard)
  • HY-182722
    UT-105
    		Degrader
    UT-105 is an orally active androgen receptor (AR) degrader. UT-105 binds to the N-terminal domain of AR and promotes its degradation. UT-105 inhibits the growth of enzalutamide-resistant breast cancer xenografts and reduces tumor cell proliferation. UT-105 can be used in the research of estrogen receptor-positive breast cancer.
    UT-105
  • HY-B0333S2
    Sulfamethizole-d4-1
    		Antagonist
    Sulfamethizole-d4-1 is the deuterium labeled Sulfamethizole (HY-B0333). Sulfamethizole is a sulfathiazole antibiotic. Sulfamethizole inhibits the synthesis of folic acid and thymine, and selectively suppresses Photobacterium phosphoreum bioluminescence. Sulfamethizole exerts antibacterial activity against Escherichia coli-mediated urinary tract infections but no activity against sulII gene-positive Escherichia coli. Sulfamethizole is applicable for the research of urinary tract infections and Photobacterium phosphoreum bioluminescence mechanisms.
    Sulfamethizole-d<sub>4</sub>-1
  • HY-W716464
    Prochloraz-d7
    Prochloraz-d7 (BTS 40542-d7) is the deuterium labeled Prochloraz (HY-B0845). Prochloraz is an imidazole antifungal. Prochloraz is as an estrogen receptor (ER) and androgen receptor (AR) antagonist and an aromatase inhibitor with IC50 values of 25 μM, 4 μM and 0.3 μM, respectively. Prochloraz is able to activate the aryl hydrocarbon receptor (AhR) having an EC50 of 1 μM.
    Prochloraz-d<sub>7</sub>
  • HY-W745855
    Androstatrione
    Androstatrione is an androgenic compound.
    Androstatrione
  • HY-106827
    Trimegestone
    Trimegestone (RU 27987) is an orally active, selective progestogen and PR ligand, with an IC50 of 7.6 nM for hPR, 4.4 nM for rabbit PR, and 3.3 nM for rat PR. Trimegestone induces Alkaline phosphatase activity. Trimegestone exhibits antiandrogenic activity (IC50 = 303 nM). Trimegestone can be used in research related to menopausal symptoms and osteoporosis.
    Trimegestone
  • HY-P4779
    Acetyl-ACTH (2-24) (human, bovine, rat)
    		Modulator
    Acetyl-ACTH (2-24) (human, bovine, rat) is a fragment of proopiomelanocortin (POMC) peptide. POMC peptides such as adrenocorticotrophin (ACTH), which is the precursor of α-MSH, is also an agonist at the MC-1 receptor.
    Acetyl-ACTH (2-24) (human, bovine, rat)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity