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-135732
    SK33
    		Antagonist 99.98%
    SK33, a trifluoromethylated enobosarm analog, is a potent, and tissue selective anti-androgen. SK33reduces androgen receptor (AR) transcriptional activity.
    SK33
  • HY-164807
    SARD279
    		Degrader
    SARD279 is a potent and selective Androgen Receptor degrader with DC50 value of 1099 nM. SARD279 can be used in prostate cancer research.(Structure Note: Pink: target protein ligand (HY-117486); Blue,: Hyt (HY-W001578); Black: linker (HY-W004896))
    SARD279
  • HY-161741
    VinclozolinM2-2204
    		Degrader 98.00%
    VinclozolinM2-2204 is a androgen receptor (AR) AUTOTAC degrader, with an DC50 of 200 nM in LNCaP prostate cancer cells. VinclozolinM2-2204 induces the formation of AR+LC3+ autophagic membranes. VinclozolinM2-2204 can be used for the research of cancer.(Pink: AR inhibitor (HY-168296); Black: linker (HY-128833); Blue: CRBN Ligand (HY-168293))
    VinclozolinM2-2204
  • HY-70002S
    Deutenzalutamide-d3
    		Antagonist 99.80%
    Deutenzalutamide (Enzalutamide-d3) is a developed deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells.
    Deutenzalutamide-d<sub>3</sub>
  • HY-101734
    Trestolone
    		99.00%
    Trestolone is a synthetic anabolic-androgenic steroid (AAS) of the nandrolone (19-nortestosterone) group.
    Trestolone
  • HY-B1095
    Chlormadinone acetate
    		Ligand 98.0%
    Chlormadinone acetate is a progestogen with potent progestogenic activity and antiandrogenic effects. Chlormadinone acetate acts on glucocorticoid receptor, progesterone receptor, androgen receptor, and GABAA receptor. Chlormadinone acetate induces endometrial proliferation in estrogen-pretreated rabbits, inhibits testosterone-stimulated growth of the prostate and seminal vesicles in castrated rats, and reduces the thymus and adrenal weights in juvenile rats. Chlormadinone acetate is applicable to research related to diseases such as depression and reproductive metabolic disorders.
    Chlormadinone acetate
  • HY-168299
    AR ligand-30
    		Ligand
    AR ligand-30 is a target protein ligand for PROTAC Bavdegalutamide (HY-138641), which can be used in prostate cancer research.
    AR ligand-30
  • HY-B1866S
    Linuron-d6
    		99.76%
    Linuron-d6 is the deuterium labeled Linuron (HY-B1866). Linuron is a phenylurea herbicide that is widely used to control the growth of grass and weeds in various agriculture crops and in orchards. Linuron is a photosystem II inhibitor. Linuron is also a competitive androgen receptor (AR) antagonist with a Ki of 100 μM. Linuron shows reproductive toxicity in animals that acts as an endocrine disruptor.
    Linuron-d<sub>6</sub>
  • HY-B0469S
    Medroxyprogesterone acetate-d3
    		98.13%
    Medroxyprogesterone acetate-d3 is deuterium labeled Medroxyprogesterone acetate. Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors.
    Medroxyprogesterone acetate-d<sub>3</sub>
  • HY-B0561S
    Spironolactone-d7
    		Antagonist 99.96%
    Spironolactone-d7 is the deuterium labeled Spironolactone. 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-d<sub>7</sub>
  • HY-W713284
    2-Ethylhexyl (E)-3-(4-(methoxy-d3)phenyl)acrylate
    		99.87%
    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-142026
    Vitisin A
    		Inhibitor
    Vitisin A ((+)-Vitisin A) is an orally active natural product with multiple pharmacological activities including anti-inflammatory, anti-tumor, anti-oxidant, anti-pathogenic microorganism, hypoglycemic and lipid-regulating, anti-osteoporotic, neuroprotective and cardiovascular protective effects. Vitisin A exhibits inhibitory effects on human AChE and MAO-B with IC50 values of 1.29 µM and 4.94 µM, respectively. Vitisin A inhibits the ERK, MAPK, NF-κB, STAT1, HMGCR and TRAF6 pathways, downregulates the related phosphorylation and protein expression, while activates the Nrf2/HO-1 pathway and upregulates p21 expression. Vitisin A induces tumor cell apoptosis and cell cycle arrest, inhibits adipogenesis and lipid accumulation, while alleviates oxidative stress, suppresses inflammatory responses, blocks hepatic fibrosis, Cuproptosis and cholesterol synthesis, and increases the expression levels of central BDNF and TrkB. Vitisin A can be used in the research of tumors, infectious diseases, metabolic diseases, bone and joint diseases, liver diseases, skin injuries, as well as neurodegenerative and cognitive dysfunction-related diseases.
    Vitisin A
  • 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-112689
    Androgen receptor antagonist 9
    		99.91%
    Androgen receptor antagonist 9 (compound 28) is an antagonist of the androgen receptor.
    Androgen receptor antagonist 9
  • HY-123012A
    Lubabegron fumarate
    		Antagonist 98.44%
    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-N12124
    Monascuspiloin
    		Inhibitor
    Monascuspiloin (Monascinol) exhibits anti-androgenic activity with an IC50 of 7 μM. Monascuspiloin inhibits viability of PC-3 and LNCaP with IC50 of 45 and 47 μM. Monascuspiloin induces apoptosis in LNCaP through inhibition of Akt/mTOR signaling pathway, induces autophagy through activation AMPK signaling pathway and arrest cell cycle at G2/M phase in PC-3. Monascuspiloin exhibits antitumor efficacy in mice.
    Monascuspiloin
  • HY-163940
    LX1
    		99.13%
    LX1 is an anti-prostate cancer compound that targets androgen receptor (AR), AR variants and steroidogenic enzyme AKR1C3. LX1 inhibits the enzymatic activity of AKR1C3, reduces the conversion of androstenedione to testosterone and reduces the expression of AR and AR-V7 and downregulates their target genes. LX1 overcomes the resistance of tumor cells to Enzalutamide (HY-70002), and the combination with Enzalutamide (HY-70002) further inhibits tumor growth.
    LX1
  • HY-W721874
    Adrenosterone-d10
    Adrenosterone-d10 ((+)-Adrenosterone-d10) is the deuterium 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-d<sub>10</sub>
  • HY-14250
    PF-998425
    		Antagonist 98.31%
    PF-998425 is a potent, selective nonsteroidal androgen receptor (AR) antagonist with an IC50 of 37 nM and 43 nM in AR binding and cellular assays, respectively. PF-998425 has low activity on common receptors and enzymes, such as progesterone receptor. PF-998425 can be used for sebum control and androgenetic alopecia research.
    PF-998425
  • HY-105318
    LGD-2226
    		Modulator 98.58%
    LGD-2226 is a selective and orally active androgen receptor modulator with an EC50 of 0.2 nM and a Ki of 1.5 nM for human androgen receptor. LGD-2226 shows tissue selectivity in animal models, with reduced effects on prostate compared to muscle. LGD-2226 can be used for muscle wasting, osteoporosis and sexual dysfunction.
    LGD-2226
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity