1. Signaling Pathways
  2. Vitamin D Related/Nuclear Receptor
  3. Androgen Receptor

Androgen Receptor

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-146397
    TD-802
    Inhibitor
    TD-802 (Compound 33c) is an androgen receptor (AR) PROTAC degrader with good microsomal stability. TD-802 has good antitumor efficacy in vivo and can be used for metastatic castration-resistant prostate cancer research.
    TD-802
  • HY-152520
    RLA-5331
    Activator
    RLA-5331 is an iron activator containing anti-androgen. RLA-5331 has anti-proliferative activity on metastatic castration-resistant prostate cancer (mCRPC) cell line.
    RLA-5331
  • HY-171049
    Androgen receptor modulator 3
    Modulator
    Androgen receptor modulator 3 is a selective modulator for androgen receptor that can be used for research of sarcopenia.
    Androgen receptor modulator 3
  • HY-B0561S2
    Spironolactone-d3-1
    Antagonist
    Spironolactone-d3-1 is 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[1][2][3].
    Spironolactone-d<sub>3</sub>-1
  • HY-19470R
    Topilutamide (Standard)
    Inhibitor
    Topilutamide (Standard) is the analytical standard of Topilutamide. This product is intended for research and analytical applications. Topilutamide is a topical nonsteroidal antiandrogen (NSAA).
    Topilutamide (Standard)
  • HY-13604S
    Cyproterone acetate-d3
    Antagonist
    Cyproterone acetate-d3 is deuterium labeled Cyproterone acetate. Cyproterone acetate is an anti-androgen (IC50=7.1 nM) and progestogen synthetic steroid. Cyproterone acetate has affinity with progesteron and with glucocorticoidal receptors[1][2].
    Cyproterone acetate-d<sub>3</sub>
  • HY-13607A
    (rel)-BMS-641988
    Antagonist
    (rel)-BMS-641988 is a relative configuration of BMS-641988. BMS-641988 is a potent nonsteroidal androgen receptor antagonist. BMS-641988 has the potential for the research of prostate cancer.
    (rel)-BMS-641988
  • HY-P2413
    Ac-PPPHPHARIK-NH2
    Inhibitor
    Ac-PPPHPHARIK-NH2 (compound S1) is a compound that inhibits the interaction between androgen receptor and Src. It can inhibit the binding of androgen or estrogen-induced receptor and Src in cancer cells, as well as the activation of related signaling pathways, and can also inhibit cell cycle progression and tumor growth.
    Ac-PPPHPHARIK-NH2
  • HY-143471
    WNY0824
    Inhibitor
    WNY0824 (PLK1/BRD4-IN-1) is an orally active dual inhibitor of PLK1 and BET protein families, with IC50 values ​​of 22, 402.5, 150.7, 103.9, and 311.9 nmol/L for PLK1, BRD2, BRD3, BRD4, and BRDT, respectively. WNY0824 induces cell cycle arrest and apoptosis by inhibiting AR- and MYC-mediated transcriptional processes. In addition, WNY0824 also inhibits tumor growth in Enzalutamide (HY-70002) resistant CRPC xenograft tumor models.
    WNY0824
  • HY-B0846S
    Dimethomorph-d8
    Dimethomorph-d8 is the deuterium labeled Dimethomorph[1]. Dimethomorph is a fungicide belongs to the fungicide group of sterol biosynthesis inhibitor. Dimethomorph can inhibit fungal cell wall formation. Dimethomorph also inhibits androgen receptor (AR) activity in MDA-kb2 cells with an IC20 of 0.263 μM[2][3][4].
    Dimethomorph-d<sub>8</sub>
  • HY-168141
    Androgen receptor antagonist 11
    Antagonist
    Androgen receptor antagonist 11 (compund N29) is a derivative of the androgen receptor (AR) antagonist M17-B15, and is a selective and orally active AR antagonist (IC50=18 nM)..
    Androgen receptor antagonist 11
  • HY-B1405R
    Dehydroisoandrosterone 3-acetate (Standard)
    Agonist
    Dehydroisoandrosterone 3-acetate (Standard) is the analytical standard of Dehydroisoandrosterone 3-acetate. This product is intended for research and analytical applications. Dehydroepiandrosterone 3-acetate is a testosterone/estrogen precursor and known modulator of vertebrate aggression.
    Dehydroisoandrosterone 3-acetate (Standard)
  • HY-125065
    MK-4541
    Modulator
    MK-4541 is an orally active and selective androgen receptor (AR) modulator. MK-4541 acts as an antagonist to inhibit 5α-reductase. MK-4541 inhibits proliferation and induces apoptosis in AR positive prostate cancer cells. MK-4541 significantly inhibited the growth of R3327-G prostate tumors in xenograft mouse model.
    MK-4541
  • HY-123308
    VPC13163
    Inhibitor
    VPC13163 is a potent androgen receptor (AR) BF3 inhibitor with an IC50 of 0.31 µM. VPC13163 has anticancer effects.
    VPC13163
  • HY-P4782
    Acetyl-ACTH (3-24) (human, bovine, rat)
    Modulator
    Acetyl-ACTH (3-24) (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 (3-24) (human, bovine, rat)
  • HY-111246
    MK-3984
    Modulator
    MK-3984 is a selective androgen receptor modulator (SARM). MK-3984 can be used for the research of muscle wasting associated with cancer.
    MK-3984
  • HY-170951
    AR antagonist 10
    Antagonist
    AR antagonist 10 (Compound Y5) is potent and orally active androgen receptor (AR) antagonist with an IC50 of 0.04 μM. AR antagonist 10 demonstrates dual mechanisms of action, antagonizes AR by disrupting AR dimerization, and induces AR degradation via the ubiquitin-proteasome pathway. AR antagonist 10 exhibits excellent activity against variant drug-resistant AR mutants. AR antagonist 10 effectively suppresses the tumor growth of the LNCaP xenograft. AR antagonist 10 is potential to be used for drug-resistant prostate cancer.
    AR antagonist 10
  • HY-159922
    AR antagonist 9
    Antagonist
    AR antagonist 9 is an orally bioavailable selective androgen receptor (AR) antagonist that exerts anticancer effects by disrupting the dimerization of AR ligand-binding domains, showing potential for overcoming drug resistance in prostate cancer (PCa). Its AR antagonistic activity has an IC50 value of 0.051 μM, comparable to Enzalutamide (HY-70002) (IC50 = 0.060 μM). AR antagonist 9 demonstrated superior efficacy against ARF876L/T877A and ARW741C mutants compared to Enzalutamide (HY-70002). Furthermore, AR antagonist 9 exhibited favorable pharmacokinetic properties, with an oral bioavailability of F = 66.24% in rats. In the LNCaP xenograft mouse model, oral administration of AR antagonist 9 significantly inhibited tumor growth. AR antagonist 9 holds promise for research into overcoming PCa drug resistance.
    AR antagonist 9
  • HY-146027
    Androgen receptor antagonist 4
    Antagonist
    Androgen receptor antagonist 4 (Compound AT2) is an androgen receptor (AR) antagonist with an IC50 of 0.15 μM. Androgen receptor antagonist 4 efficiently antagonizes AR transcriptional activity, suppresses downstream target gene of AR, and blocks the DHT-induced AR nuclear translocation. Androgen receptor antagonist 4 shows anticancer activities.
    Androgen receptor antagonist 4
  • HY-111044
    (+)-JNJ-37654032
    Modulator
    (+)-JNJ-37654032 is an orally active and selective androgen receptor modulator. (+)-JNJ-37654032 can be used in the study of muscle-wasting diseases.
    (+)-JNJ-37654032
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity