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-N2908R
    Atraric acid (Standard)
    		Antagonist
    Atraric acid (Standard) is the analytical standard of Atraric acid. This product is intended for research and analytical applications. Atraric acid (Methyl atrarate) is a specific androgen receptor (AR) antagonist with anti-inflammatory and anticancer effects. Atraric acid represses the expression of the endogenous prostate specific antigen gene in both LNCaP and C4-2 cells. Atraric acid can also inhibit the synthesis of NO and cytokine, and suppress the MAPK-NFκB signaling pathway. Atraric acid can be used to research prostate diseases and inflammatory diseases[1][2].
    Atraric acid (Standard)
  • HY-115282
    JNJ-63576253 free base
    		Antagonist
    JNJ-63576253 (TRC-253) free base 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 free base can be used for the research of castration-resistant prostate cancer (CRPC).
    JNJ-63576253 free base
  • HY-111421
    ODM-204
    		Inhibitor
    ODM-204 is novel nonsteroidal dual inhibitor of both androgen receptor and CYP17A1 enzyme, with IC50s of 80 nM and 22 nM, respectively.
    ODM-204
  • HY-16247
    Apoptone
    		Inhibitor
    Apoptone (HE3235) is an orally active 3β-androstanediol analog. Apoptone reduces the expression of androgen receptor (Androgen receptor) and decreases intratumoral androgen levels. Apoptone exhibits anticancer activity against castration-resistant prostate cancer.
    Apoptone
  • HY-13702S
    Nilutamide-d6
    		Antagonist 99.77%
    Nilutamide-d6 (Nilandron-d6) is the deuterium labeled Nilutamide. Nilutamide (Nilandron) is a non-steroidal anti-androgen agent proposed in the research of metastatic prostatic carcinoma.
    Nilutamide-d<sub>6</sub>
  • HY-162423
    CYB210010
    		Agonist
    CYB210010 is an orally bioavailable, long-acting serotonin 5-HT2 receptor agonist that selectively targets 5-HT2A and 5-HT2C receptors (EC50: 4.1 n, 7.3 nM). CYB210010 can enter the central nervous system, cause a head twitch response (HTR), and is not prone to behavioral tolerance during chronic administration.
    CYB210010
  • HY-183667
    JNJ-pan-AR
    		Inhibitor
    JNJ-pan-AR is an orally active androgen receptor (AR) inhibitor with an IC50 of 19 nM and a Ki of 8.4 nM against human wild-type AR. JNJ-pan-AR abolishes androgen-induced KLK2 and KLK3 mRNA expression and reduces androgen-dependent colony formation in prostate cancer cells. JNJ-pan-AR blocks AR nuclear translocation, inhibits PSA protein expression, and represses the growth of AR-dependent tumor cells and ARF877L-driven tumor xenografts. JNJ-pan-AR blocks transactivation and signaling of wild-type AR and various mutant AR variants. JNJ-pan-AR is applicable for research on castration-resistant prostate cancer.
    JNJ-pan-AR
  • HY-403733B
    (+)-JJ-450
    		Antagonist
    (+)-JJ-450 is a non-competitive antagonist targeting the androgen receptor (AR) that inhibits AR nuclear localization and transcriptional activity in the absence of androgen. (+)-JJ-450 is less active than (-)-JJ-450 (HY-403733A) in inhibiting prostate-specific antigen (PSA) expression in LN95 cells, possibly because (+)-JJ-450 targets the ligand binding domain (LBD) of AR. (+)-JJ-450 inhibits the transcriptional activity of AR and its splice variants (e.g., ARv7) by promoting the degradation of unliganded AR in the nucleus and reducing the binding of AR to androgen response elements (AREs). (+)-JJ-450 can be used in castration-resistant prostate cancer (CRPC) studies that are resistant to enzalutamide (MDV3100) (HY-70003).
    (+)-JJ-450
  • HY-173640
    ID11916
    		Antagonist
    ID11916 is an orally active androgen receptor (AR) antagonist and a phosphodiesterase 5 (PDE5) inhibitor. ID11916 blocks androgen binding to AR, nuclear translocation, and androgen-dependent transcriptional activity of AR, while increasing intracellular cGMP levels and activating PKG via inhibition. ID11916 shows potent anti-cancer effect in prostate cancer cell lines VCaP and 22Rv1 and in AR-positive breast cancer cell lines SK-BR-3.
    ID11916
  • HY-135473
    Chlormadinone
    		Inhibitor 98.09%
    Chlormadinone is an orally active anti-androgen agent. Chlormadinone improves intermittency, terminal dribbling, and urinary stream size and force. Chlormadinone can be used for the research of benign prostatic hyperplasia.
    Chlormadinone
  • HY-W411296
    6α-Chloro testosterone
    6α-Chloro testosterone is an anabolic androgenic steroid.
    6α-Chloro testosterone
  • HY-111231
    CH4933468
    		Antagonist
    CH4933468 is a thiohydantoin derivative, shows androgen receptor (AR) pure antagonist activity in vitro. CH4933468 inhibits AR-mediated transactivation and proliferation of LNCaP and LNCaP-BC2 cells. CH4933468 can be used for castration-resistant prostate cancer (CRPC) research.
    CH4933468
  • HY-172954
    Androgen receptor ligand 1
    Androgen receptor ligand 1 is an androgen receptor (AR) ligand. Androgen receptor ligand 1 binds to CRBN E3 ligase via a linker to form an AR PROTAC degrader. Androgen receptor ligand 1 can be used in the study of prostate cancer.
    Androgen receptor ligand 1
  • HY-153276
    Androgen receptor-IN-5
    		Inhibitor
    Androgen receptor-IN-5 is an androgen receptor inhibitor with potent anticancer effects. Androgen receptor-IN-5 also inhibits the production of IL-17A, IL- 17F and INF-γ (WO2023281097A1,Example 1/1).
    Androgen receptor-IN-5
  • HY-P991673
    Asedebart
    		Antagonist
    Asedebart is a CHO-expressed human antibody that targets Adrenocorticotropic hormone (ACTH). Asedebart blocks the binding of ACTH to its receptor through antagonism. Asedebart has huIgG1 heavy chain and huκ light chain, with a predicted molecular weight (MW) of 145 kDa. The isotype control for Asedebart can refer to Human IgG1 kappa, Isotype Control (HY-P99001). Asedebart can be used for inflammatory diseases such as psoriasis and ulcerative colitis research.
    Asedebart
  • HY-149914
    WCA-814
    		Degrader
    WCA-814 is an androgen receptor (AR) antagonist-Hsp90 inhibitor conjugate. WCA-814 induces the degradation of full-length and AR-V7. WCA-814 has cytotoxic effect in prostatic cancer cells (IC50: 171.2 nM, 26.5 nM for LNCaP, 22Rv1 cell).
    WCA-814
  • HY-173372
    PROTAC AR Degrader-10
    		Degrader
    PROTAC AR Degrader-10 (GT19) is a protein degrader targeting the androgen receptor (AR) with a DC50 value ≤100 nM. PROTAC AR Degrader-10 can be used for prostate cancer study. (Structure Note: Pink: target protein ligand (HY-173373); Blue: E3 ligase ligand (HY-138793); Black: linker) .
    PROTAC AR Degrader-10
  • HY-181727
    AR/AR-V7 degrader-1
    		Degrader
    AR/AR-V7 degrader-1 is an orally active AR and AR-V7 degrader. AR/AR-V7 degrader-1 disrupts the interaction between AR/AR-V7 and HSP90, leading to their ubiquitination and degradation in castration-resistant prostate cancer cells. AR/AR-V7 degrader-1 regulates the expression of cell cycle-related proteins in prostate cancer cells (downregulates CDK4, CDK6, Cyclin D1, Cyclin E1; upregulates P21) and induces G0/G1 phase arrest. AR/AR-V7 degrader-1 inhibits the proliferation and migration of prostate cancer cells. AR/AR-V7 degrader-1 suppresses the growth of castration-resistant prostate cancer tumors in nude mice and induces the degradation of AR and AR-V7 in tumor tissues. AR/AR-V7 degrader-1 is applicable to the research of castration-resistant prostate cancer.
    AR/AR-V7 degrader-1
  • HY-172624
    AR antagonist 14
    		Antagonist
    AR antagonist 14 is is a PROTAC target protein ligand (Ligands for Target Protein for PROTAC). AR antagonist 14 can be combined with VH 101-amide-piperidine-Pip-alkyne (HY-172625) to synthesize PROTAC degraders (ARD-69 (HY-114402)).
    AR antagonist 14
  • HY-125627
    CP-394531
    		Antagonist
    CP-394531 is an efficient and highly selective non-steroidal glucocorticoid receptor (GR) antagonist, with a Ki value of 0.1 nM. CP-394531 has a weak binding to androgen receptor (AR) (Ki = 130 nM), and has almost no effect on progesterone receptor (PR) and estrogen receptors (ERα, ERβ). CP-394531 completely blocks the half-maximal agonistic effect induced by Dexamethasone (HY-14648G), with a Kif of 4.1 nM. CP-394531 can be used to study various diseases such as diabetes, obesity, depression, neurodegenerative diseases, glaucoma and Cushing's disease.
    CP-394531
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity