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-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-N12124
    Monascuspiloin
    		Inhibitor
    Monascuspiloin (Monascinol) exhibits anti-androgenic activity with an IC50 of 7 μM. Monascuspiloin inhibits viability of PC-3 and LNCaP with IC50 of 45 and 47 μM. Monascuspiloin induces apoptosis in LNCaP through inhibition of Akt/mTOR signaling pathway, induces autophagy through activation AMPK signaling pathway and arrest cell cycle at G2/M phase in PC-3. Monascuspiloin exhibits antitumor efficacy in mice.
    Monascuspiloin
  • HY-167655
    KF-19418
    		Inhibitor
    KF-19418 is an anti-androgen antisense oligonucleotide (ASO) and a hair follicle stimulator. KF-19418 directly stimulated hair follicle in vitro and has hair growth promoting activities in vivo.
    KF-19418
  • 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-13273S
    Ostarine-d4
    		Modulator
    Ostarine-d4 is a deuterated labeled Ostarine.
    Ostarine-d<sub>4</sub>
  • HY-W721874
    Adrenosterone-d10
    Adrenosterone-d10 ((+)-Adrenosterone-d10) is the deuterium 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-d<sub>10</sub>
  • HY-116214S
    Cyprodinil-d5
    		Agonist
    Cyprodinil-d5(CGA-219417-d5) is the deuterium labeled Cyprodinil (HY-116214). Cyprodinil (CGA-219417) is a broad-spectrum anilinopyrimidine fungicide and an activator of the aryl hydrocarbon receptor. Cyprodinil also has anti-androgenic and androgenic activities. Cyprodinil can inhibit the biosynthesis of methionine in plant-pathogenic fungi and protect fruits and vegetables from a variety of pathogens.
    Cyprodinil-d<sub>5</sub>
  • HY-135331S
    N-Desmethyl-Apalutamide-15N,d4
    		Antagonist
    N-Desmethyl-Apalutamide-15N,d4 is the 15N and deuterium labeled isotope of N-Desmethyl-Apalutamide (HY-135331). 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-<sup>15</sup>N,d<sub>4</sub>
  • HY-P3604
    LH-RH II (chicken)
    		Modulator
    LH-RH II (chicken) is one of the two forms of luteinizing hormone-releasing hormone (LHRH) the hypothalamus of the domestic hen, which are structural variants of mammalian LHRH. LH-RH II (chicken) enhances gonadotrophin release in the domestic chicken.
    LH-RH II (chicken)
  • HY-174908
    SJL2-1
    		Inhibitor
    SJL2-1 is a PRMT5 inhibitor, with an IC50 of 1.56 μM. SJL2-1 suppresses proliferation, migration, and invasion in prostate cancer cells. SJL2-1 promotes apoptosis and blocks the cell cycle at the G0/G1 phase. SJL2-1 can target the binding of PRMT5 in cells and inhibit the methylation and expression of the androgen receptor. SJL2-1 can be used for the study of early androgen-sensitive prostate cancer and advanced castration-resistant prostate cancer (CRPC).
    SJL2-1
  • HY-160692
    AR antagonist 7
    		Antagonist
    AR antagonist 7 (86) is an androgen receptor (AR) antagonist that can be used in the research of hair loss.
    AR antagonist 7
  • HY-167878
    Pentomone
    Pentomone (LY-113935), an antiandrogen compound, is a prostate growth inhibitor.
    Pentomone
  • HY-123047R
    Tibolone (Standard)
    		Agonist
    Tibolone (Standard) is the analytical standard of Tibolone. This product is intended for research and analytical applications. Tibolone is a broad spectrum gonadal steroid agonist with progestagenic, androgenic, and estrogenic activities. Tibolone can be used for postmenopausal osteoporosis research.
    Tibolone (Standard)
  • HY-123310
    JNJ-26146900
    		Antagonist
    JNJ-26146900 is a potent and orally active androgen receptor antagonist with a Ki value of 400nM for rat AR. JNJ-26146900 is a nonsteroidal androgen receptor (AR) ligand. JNJ-26146900 reduces prostate tumor size and prevents bone loss. JNJ-26146900 can be used in research of cancer.
    JNJ-26146900
  • HY-146494
    Androgen receptor antagonist 5
    		Antagonist
    Androgen receptor antagonist 5 (compound 42f) is a potent androgen receptor (AR) antagonist with an IC50 value of 6.17 μM. Androgen receptor antagonist 5 can effectively impair AR nuclear translocation, reducing the levels of nuclear AR, and disrupts AR-mediated gene regulation. Androgen receptor antagonist 5 has antiproliferative activity against LNCaP and exhibits antitumor activity in LNCaP xenograft tumor mice model. Androgen receptor antagonist 5 can be used for researching prostate cancer.
    Androgen receptor antagonist 5
  • HY-169385
    ATC-324
    		Degrader
    ATC-324 is an bivalent AR (Androgen Receptor) degrader based on the protein degradation technology platform AUTOphagy-TArgeting Chimera (AUTOTAC). ATC-324 induces the formation of AR/p62 complex, leading to autophagy-lysosomal degradation of AR. ATC-324 can reduce nuclear AR levels and downregulate target gene expression of AR and AR-v7, and also has a degradation effect on common AR mutants in PCa. ATC-324 is composed of target-binding ligand (TBL) Enzalutamide (HY-70002) and p62/SQSTM1 autophagy-targeting ligand (ATL) YT 6-2 analog-1 (HY-169386), connected by Boc-NH-PEG4-CH2CH2NH2 (HY-W008352). Among them, the active control of the target protein ligand is Enzalutamide carboxylic acid (HY-70002B), and the conjugate composed of the autophagy-targeting ligand and the linker is YT 6-2-PEG3-C2-NH2 (HY-169387).
    ATC-324
  • HY-101734
    Trestolone
    		99.00%
    Trestolone is a synthetic anabolic-androgenic steroid (AAS) of the nandrolone (19-nortestosterone) group.
    Trestolone
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity