2. シグナル伝達
  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).

製品番号 製品名 製品効果 純度 構造式
  • HY-W759219
    Adrenosterone-13C3
    Adrenosterone-13C3 ((+)-Adrenosterone-13C3) is the 13C-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-<sup>13</sup>C<sub>3</sub>
  • HY-P11443
    SRC2-2 peptide Ligand
    SRC2-2 peptide is a a coactivator-derived mimic targeting androgen receptor (AR) ligand. SRC2-2 peptide is promising for research of prostate cancer.
    SRC2-2 peptide
  • HY-178938
    AR Degrader-3 Degrader
    AR Degrader-3 is an orally active molecular glue that targets AR/ARV7 and induces the degradation of AR and ARV7 through the ubiquitin-proteasome pathway (UPP). AR Degrader-3 directly interacts with the ligand-binding domain (LBD) and the N-terminal domain (NTD) of AR. AR Degrader-3 effectively suppresses the transcriptional activity of wild-type AR (AR-WT), AR mutants, and ARV7. AR Degrader-3 downregulates the mRNA and protein levels of downstream AR target genes, thereby overcoming antiandrogen resistance mediated by ARV7 and AR point mutations. AR Degrader-3 induces apoptosis in Enzalutamide (HY-70002) (ENZa)-resistant cells and increases cleaved caspase-3 protein levels. AR Degrader-3 can be used for the study of castration-resistant prostate cancer (CRPC).
    AR Degrader-3
  • HY-400666A
    AR ligand-44 TFA
    AR ligand-44 TFA is an androgen receptor ligand that can be used in the synthesis of PROTACs, such as ARD-2051 (HY-149862).
    AR ligand-44 TFA
  • HY-16060S3
    Apalutamide-d7 Antagonist
    Apalutamide-d7 is deuterated labeled Apalutamide (HY-16060). Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM.
    Apalutamide-d<sub>7</sub>
  • HY-W744741
    Lupeol-d3
    Lupeol-d3 is the deuterium labeled Lupeol (HY-N0790). Lupeol 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-d<sub>3</sub>
  • HY-180409
    YM580 Antagonist
    YM580 is a potent, orally active and selective Androgen Receptor (AR) antagonist (IC50 = 0.11 μM, hAR Ki = 4.6 nM, rAR Ki = 6.2 nM). YM580 exhibits good selectivity over PR, GR, and ERα (Kis > 3300 nM). YM580 decreases ventral prostate weight in mature intact rats dose-dependently without affecting serum testosterone levels. YM580 can be used for the research of prostate cancer.
    YM580
  • HY-122894
    Ch-319 Inhibitor
    Ch-319 is a Triphenyltin (IV) carboxylate derivative. Ch-319 reduces androgen receptor expression, AKT and PRAS40 phosphorylation levels, and increases FOXO3a expression. Ch-319 increases Apoptosis. Ch-319 can be used in the research of prostate cancer.
    Ch-319
  • HY-181670
    WH23 Inhibitor
    WH23 is a dehydrogenase/reductase SDR family member 11 (DHRS11) inhibitor with IC50 values of 0.037 μM. WH23 binds to DHRS11, forming a hydrogen bond with the enzyme’s His210 residue. WH23 suppresses androgen receptor mRNA and protein expression, reduces c-Myc expression, and inhibits cancer cell proliferation. WH23 inhibits PI3K/AKT signaling by reducing phosphorylation of PDK1, AKT, mTOR, and ERK. WH23 enhances Capivasertib (HY-15431)-induced cytotoxicity and apoptosis. WH23 can be used for the research of luminal androgen receptor-positive triple-negative breast cancer.
    WH23
  • HY-155543
    Anticancer agent 135 Antagonist
    Anticancer agent 135 (compound 26h) is a potent androgen receptor (AR) antagonist. Anticancer agent 135 can effectively block AR nuclear translocation and inhibit AR/AR-V7 heterodimerization, thereby inhibiting downstream gene transcription. Anticancer agent 135 displays potent robust efficacy in prostate cancer xenograft models.
    Anticancer agent 135
  • HY-Y0978S2
    Boc-Glycine-2-13C Antagonist
    Boc-Glycine-2-13C is a 13C-labeled Boc-Glycine (HY-Y0978). Boc-Glycine is a Glycine (HY-Y0966) derivative.
    Boc-Glycine-2-<sup>13</sup>C
  • HY-113289R
    Brassicasterol (Standard) Inhibitor
    L-Ornithine (hydrochloride) (Standard) is the analytical standard of L-Ornithine (hydrochloride). This product is intended for research and analytical applications. L-Ornithine hydrochloride is a non-proteinogenic amino acid, is mainly used in urea cycle removing excess nitrogen in vivo. L-Ornithine hydrochloride shows nephroprotective.
    Brassicasterol (Standard)
  • HY-120703
    RU 58642 Inhibitor
    RU 58642 is an orally active non-steroidal antiandrogen, which displays a strong and selective affinity for androgen receptor.
    RU 58642
  • HY-167655
    KF-19418 Inhibitor
    KF-19418 is a hair follicle stimulator with hair growth promoting activity. KF-19418 stimulates proliferation of cultured hair bulb cells from newborn mice. KF-19418 accelerates hair regrowth in hair-clipped mouse alopecia model following topical application. KF-19418 can be used for the research of alopecia.
    KF-19418
  • HY-W657887
    GSK-3β/G9a-IN-1 Inhibitor
    GSK-3β/G9a-IN-1 (Compound T2) is an orally active, selective, blood-brain-barrier permeable, competitive G9a (substrate-competitive, IC50: 1.1 μM) and GSK-3β (ATP competitive, IC50: 0.8 μM) inhibitor. GSK-3β/G9a-IN-1 is a potent H3K9me2 inhibitor that reshapes chromatin landscape. GSK-3β/G9a-IN-1 lowers tau phosphorylation, reduces Aβ aggregation. GSK-3β/G9a-IN-1 displays inhibition toward glucocorticoid receptor, androgen receptor, and alpha-2A adrenergic receptor. GSK-3β/G9a-IN-1 also upregulates SAGA complex members such as Eny2 and Sgf29. GSK-3β/G9a-IN-1 markedly improves memory, restores social behaviors, and increases synaptic complexity in late-onset Alzheimer’s disease.
    GSK-3β/G9a-IN-1
  • HY-157455
    AR antagonist 5
    AR antagonist 5 (compound 30a) is a selective androgen receptor (AR) antagonist with an IC50 value of 134.8 nM. AR antagonist 5 has favorable pharmacokinetic properties and shows a high skin exposure and low plasma exposure[1.
    AR antagonist 5
  • HY-174377
    PeS-9 Degrader

    PeS-9 is an Androgen Receptor (AR) degrader that induces androgen receptor degradation PeS-9 induces mitochondrial and ER stress by promoting cytotoxic ROS production, leading to the release of mitochondrial cytochrome C and AIF. PeS-9 subsequently activates caspases-9 and -3, causing DNA fragmentation and apoptotic cell death. PeS-9 has anticancer activity against prostate cancer and exerts in vivo antitumor and antimetastatic activity with minor side effects. PeS-9 can be used for the study of targeting monotherapy against GLUT-1-overexpressing tumors.
    PeS-9
  • HY-148777
    A031 Degrader
    A031 is a highly effective PROTAC androgen receptor (AR) degrader with an IC50 value less than 0.25 μM for AR protein degradation. A031 has an inhibitory effect on tumor growth in zebrafish with human prostate cancer (VCaP).
    A031
  • HY-P10248
    Atriopeptin I (rat, mouse) Activator
    Atriopeptin I rat, mouse is an atrial natriuretic peptide, which stimulates the testosterone production with half-maximum stimulation of 38 nM.
    Atriopeptin I (rat, mouse)
  • HY-156059
    NEP28 Modulator
    NEP28 is a selective androgen receptor modulator with an EC50 of 2.90 nM in 22RV1 cells. NEP28 increases the activity of Aβ-degrading enzyme neprilysin. NEP28 is efficacious in muscle and brain without serious side effects on prostate in rats. NEP28 can be used for osteoporosis, sarcopenia, and Alzheimer's disease research.
    NEP28
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製品番号 製品名 / Synonyms Application Reactivity