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-N7043
    Isosilybin A
    		Inhibitor 99.63%
    Isosilybin A is a PPARγ agonist that can be isolated from silymarin. Isosilybin A activates extrinsic and intrinsic pathways of apoptosis through targeting of the Akt-NF-kB-AR axis. Isosilybin A can relieve the inflammatory response in the rosacea model via inhibiting Erk and p38 signaling pathways and M1 macrophage polarization, with its targets related to RELA and VEGFA. Isosilybin A has anti-prostate cancer (PCA) activity[1][2][3].
    Isosilybin A
  • 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-160777
    VNPP433-3β
    		Degrader 98.01%
    VNPP433-3β (Galeterone 3β-imidazole) is an orally active molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. VNPP433-3β induces cell apoptosis. VNPP433-3β inhibits tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β can be used for the study of castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC).
    VNPP433-3β
  • 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-15758R
    3,3'-Diindolylmethane (Standard)
    		Antagonist
    3,3'-Diindolylmethane (Standard) is the analytical standard of 3,3'-Diindolylmethane. This product is intended for research and analytical applications. 3,3'-Diindolylmethane is a strong, pure androgen receptor (AR) antagonist.
    3,3'-Diindolylmethane (Standard)
  • HY-139623
    A4B17
    		Inhibitor 99.94%
    A4B17 is an androgen receptor N-terminal inhibitor for researching androgen-responsive prostate cancer.
    A4B17
  • HY-B1405
    Dehydroisoandrosterone 3-acetate
    		Agonist 98.0%
    Dehydroepiandrosterone 3-acetate is a testosterone/estrogen precursor and known modulator of vertebrate aggression.
    Dehydroisoandrosterone 3-acetate
  • HY-139659
    ARD-61
    		Inhibitor 99.57%
    ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice. ARD-61 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    ARD-61
  • HY-W041703
    6-Amino-5-bromoquinoxaline
    		Antagonist 99.83%
    6-Amino-5-bromoquinoxaline is a 2-(arylamino)imidazole derivative and a precursor of α1- and α2-androgen receptor antagonists.
    6-Amino-5-bromoquinoxaline
  • HY-120018
    VPC-13566
    		Inhibitor 99.92%
    VPC-13566, a BF3-specific small molecule, is an androgen receptor (AR) inhibitor. VPC-13566 is effective in inhibiting AR transcriptional activity in vitro as well as the growth of AR-dependent PCa cell lines. VPC-13566 can be used as a chemical probe to help identify unknown AR partners.VPC-13566 can be used for the research of cancer.
    VPC-13566
  • HY-163340
    GA32
    		Inhibitor 99.67%
    GA32 (compound 58r) is potent androgen receptor (AR)/glucocorticoid receptor (GR) dual inhibitor with IC50 values of 0.13 μM and 0.83 μM for AR and GR, respectively. GA32 inhibits the proliferation of Enzalutamide (HY-70002) resistance castration-resistant prostate cancer both in vitro and in vivo.
    GA32
  • HY-13607
    BMS-641988
    		Antagonist 99.70%
    BMS-641988 (compound 23) is an oral active nonsteroidal androgen receptor antagonist with the Ki of 1.7 nM. BMS-641988 shows anticancer activity.
    BMS-641988
  • HY-103576
    LGD-3303
    		Modulator 99.57%
    LGD-3303 is a selective androgen receptor modulator (SARM).
    LGD-3303
  • HY-159639
    BAY-2925976
    		Inhibitor 99.14%
    BAY-2925976 is an α2C adrenergic receptor (ARα2C) antagonist that can be used for the study of obstructive sleep apnea (OSA).
    BAY-2925976
  • HY-130845A
    AR antagonist 1 hydrochloride
    		Antagonist 99.53%
    AR antagonist 1 (compound 29) hydrochloride is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020).
    AR antagonist 1 hydrochloride
  • HY-W011927R
    4,4'-Sulfonyldiphenol (Standard)
    		Inhibitor
    4,4'-Sulfonyldiphenol (Bisphenol S; Bis(4-hydroxyphenyl) sulfone) (Standard) is the analytical standard of 4,4'-Sulfonyldiphenol (HY-W011927). This product is intended for research and analytical applications. 4,4'-Sulfonyldiphenol, a substitute for Bisphenol A (HY-18260), is widely used in industrial and consumer products. 4,4'-Sulfonyldiphenol is an estrogen receptor (ER) agonist and can competitively bind to thyroid hormone receptors (TR) with IC50 values for TRα and TRβ are 2650 μM and 2294 μM respectively, thereby affecting breast development and reducing the expression of androgen receptor (AR) in fetal testes. 4,4'-Sulfonyldiphenol promotes the progression of glioblastoma by upregulating the EZH2 mediated PI3K/AKT/mTOR pathway. Under chronic exposure, 4,4'-Sulfonyldiphenol can cause significant lipid deposition and dyslipidemia in the mouse liver by upregulating JunB and Atf3, and has a role in causing obesity at low doses. 4,4'-Sulfonyldiphenol induces intestinal inflammation by altering the intestinal microbiome. 4,4'-Sulfonyldiphenol accelerates the progression of atherosclerosis in zebrafish embryo larvae.
    4,4'-Sulfonyldiphenol (Standard)
  • HY-164552
    ZNU-IMB-Z15
    		Antagonist 99.03%
    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
  • HY-135794S
    11-Ketodihydrotestosterone-d3
    		Agonist ≥99.90%
    11-Ketodihydrotestosterone-d3 is the deuterium labeled 11-Ketodihydrotestosterone. 11-Ketodihydrotestosterone (11-KDHT; 5α-Dihydro-11-keto testosterone) is an endogenous steroid and a metabolite of 11β-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a potent androgen receptor (AR) agonist with a Ki of 20.4 nM and an EC50 of 1.35 nM for human AR. 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostate cancer cells.
    11-Ketodihydrotestosterone-d<sub>3</sub>
  • HY-152844
    Faznolutamide
    		Inhibitor 98.85%
    Faznolutamide is an antiandrogen agent.
    Faznolutamide
  • HY-103246
    TFM-4AS-1
    		99.96%
    TFM-4AS-1 is a selective androgen receptor modulator (SARM), and a potent androgen receptor (AR) ligand with an IC50 of 38 nM. TFM-4AS-1 is a gene-selective agonist.
    TFM-4AS-1
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity