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-176067
    LO-4-25
    		Degrader
    LO-4-25 is a covalent degrader targeting the androgen receptor (AR) and its truncated variant AR-V7. LO-4-25 covalently binds to the E3 ubiquitin ligase CUL4 DCAF16, promoting the ubiquitination of AR and AR-V7, which subsequently are recognized and degraded by the proteasome, reducing the protein levels of AR and AR-V7 in cells. LO-4-25 is promising for research of androgen-independent prostate cancers.
    LO-4-25
  • HY-100348R
    EPI-001 (Standard)
    		Inhibitor
    EPI-001 (Standard) is the analytical standard of EPI-001. This product is intended for research and analytical applications. EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer.
    EPI-001 (Standard)
  • HY-160547
    PROTAC AR Degrader-5
    		Inhibitor
    PROTAC AR Degrader-5 (compound A46) is a potent AR PROTACs degrader with an IC50 value of 49 nM. PROTAC AR Degrader-5 inhibits sebaceous plaque and induces hair regeneration (Pink: ligand for target protein (HY-169967); black: linker (HY-169966); Blue: E3 ligase ligand (HY-125845)).
    PROTAC AR Degrader-5
  • HY-103577
    LG-121071
    		Modulator
    LG-121071 is an orally active and selective androgen receptor modulator with a Ki of 17 nM.
    LG-121071
  • HY-B1866S
    Linuron-d6
    Linuron-d6 is the deuterium labeled 3-​Bromo-​L-​tyrosine[1].
    Linuron-d<sub>6</sub>
  • HY-P4413
    (Des-Glu5)-ACTH (1-24) (human, bovine, rat)
    (Des-Glu5)-ACTH (1-24) (human, bovine, rat) is an analogue of Adrenocorticotropic hormone (ACTH; HY-106373). ACTH is a polypeptide tropic hormone produced by the anterior pituitary gland, regulating cortisol and androgen production.
    (Des-Glu5)-ACTH (1-24) (human, bovine, rat)
  • HY-P4784
    Acetyl-ACTH (4-24) (human, bovine, rat)
    		Modulator
    Acetyl-ACTH (4-24) (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 (4-24) (human, bovine, rat)
  • HY-N0790R
    Lupeol (Standard)
    		Inhibitor
    Lupeol (Standard) is the analytical standard of Lupeol. This product is intended for research and analytical applications. Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic?triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent?androgen receptor (AR)?inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC).
    Lupeol (Standard)
  • HY-N6714R
    Alternariol (Standard)
    		Inhibitor
    Alternariol (Standard) is the analytical standard of Alternariol. This product is intended for research and analytical applications. 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 (Standard)
  • HY-159106
    MeSeI
    		Modulator
    MeSeI exhibits a weak inhibitory activity against monoamine oxidase MAO-A and MAO-B (IC50=198.8 µM). MeSeI regulates dopamine receptor D2 and norepinephrine receptor α2, β1, and exhibits antidepressant-like effect in mice. MeSeI is orally active.
    MeSeI
  • HY-N7045R
    Isosilybin B (Standard)
    		Inhibitor
    Isosilybin B (Standard) is the analytical standard of Isosilybin B (HY-N7045). This product is intended for research and analytical applications. Isosilybin B is a flavonolignan. Isosilybin B can be isolated from Silybum marianum. Isosilybin B can regulate cell cycle-related proteins (e.g., reduce cyclins (D3, D1, A, E), Cdk4, Cdk2, Cdc25A), and activate Caspases (Caspase-9 and Caspase-3). Isosilybin B can promote Apoptosis, reduce androgen receptor (AR) and PSA. Isosilybin B has anticancer activity against prostate cancer.
    Isosilybin B (Standard)
  • HY-118409
    VPC-3033
    		Antagonist
    VPC-3033 is an androgen receptor antagonist. VPC-3033 has a strong androgen DHT replacement potency (IC50: 0.625-2.5 μM), can effectively inhibit androgen receptor transcriptional activity (IC50=0.3 μM), and has a strong androgen receptor degradation ability. In addition, VPC-3033 exhibits significant anti-androgen receptor activity against prostate cancer cells resistant to Enzalutamide (HY-70002).
    VPC-3033
  • HY-123047S
    Tibolone-d5
    		Agonist
    Tibolone-d5 is deuterium labeled Tibolone. Tibolone is a broad spectrum gonadal steroid agonist with progestagenic, androgenic, and estrogenic activities. Tibolone can be used for postmenopausal osteoporosis research.
    Tibolone-d<sub>5</sub>
  • HY-135473R
    Chlormadinone (Standard)
    		Inhibitor
    Chlormadinone (Standard) is the analytical standard of Chlormadinone. This product is intended for research and analytical applications. Chlormadinone is an antiandrogen drug. Chlormadinone combined with Tamsulosin shows greater improvement in subjective symptoms of BPH.
    Chlormadinone (Standard)
  • HY-111309
    LGD-2941
    		Modulator
    LGD-2941 is an orally active, potent and selective androgen receptor modulator. LGD-2941 shows excellent anabolic activity in muscle with reduced effect on the prostate in a rat model of hypogonadism. LGD-2941 also improves bone strength in a rat model of post-menopausal osteoporosis.
    LGD-2941
  • HY-B1986R
    p,p'-DDE (Standard)
    		Antagonist
    p,p'-DDE (Standard) is the analytical standard of p,p'-DDE. This product is intended for research and analytical applications. p,p'-DDE (4,4'-DDE) is the major and persistent metabolite of DDT. p,p'-DDE is a orally active androgen receptor antagonist with an IC50 of 5 μM and a Ki of 3.5 μM. p,p'-DDE can affect the development and function of the male reproductive system. Additionally, high serum concentrations of p,p'-DDE may be a risk factor for type 2 diabetes in women.
    p,p'-DDE (Standard)
  • HY-16060R
    Apalutamide (Standard)
    		Antagonist
    Apalutamide (Standard) is the analytical standard of Apalutamide. This product is intended for research and analytical applications. Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM.
    Apalutamide (Standard)
  • HY-B2044
    Bromopropylate
    		Inhibitor
    Bromopropylate is a pesticide with moderate anti-androgenic activities.
    Bromopropylate
  • HY-176068
    3-Cl-Pyridine-amide-acrylaldehyde-piperazine
    3-Cl-Pyridine-amide-acrylaldehyde-piperazine is a synthetic intermediate of LO-4-25 (HY-176067). LO-4-25 is an androgen receptor (AR) DNA binding domain ligand linked via a linker to the truncated fumaramide handle. LO-4-25 shows robust degradation of both AR and AR-V7 in 22Rv1 cells.
    3-Cl-Pyridine-amide-acrylaldehyde-piperazine
  • HY-164552
    ZNU-IMB-Z15
    		Antagonist
    ZNU-IMB-Z15 (Compound Z15) is an antagonist of the androgen receptor (AR) and also a selective degrader of AR and ARV7. ZNU-IMB-Z15 can directly bind to the ligand-binding domain (LBD) and activation function-1 region of AR, and promote AR degradation through the proteasome pathway. ZNU-IMB-Z15 effectively inhibits the transcriptional activity of AR, AR mutants, and AR splice variants (ARVs), downregulating the mRNA and protein levels of AR downstream target genes, thereby overcoming the resistance to second-generation antiandrogen drugs induced by AR LBD mutations, AR amplification, and ARVs in castration-resistant prostate cancer (CRPC). ZNU-IMB-Z15 can inhibit the proliferation of AR-positive CRPC cell lines and induce their apoptosis, demonstrating anticancer activity both in vivo and in vitro.
    ZNU-IMB-Z15
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity