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

Androgen Receptor

Androgen Receptor

Related Products

PDF 1.49 MB

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-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-173373
    AR ligand-39
    		Ligand
    AR ligand-39, an androgen receptor (AR) ligand, is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). AR ligand-39 can be used for synthesis PROTAC AR Degrader-10 (HY-173372).
    AR ligand-39
  • HY-403733C
    JJ-450
    		Antagonist
    JJ-450 is a non-competitive antagonist androgen receptor (AR) that inhibits the transcriptional activity of wild-type AR and mutant ARF876L. JJ-450 has an IC50 of approximately 1-10 μM in inhibiting AR transcriptional activity in PC3 cells. It is selective for AR binding and does not compete with androgens for binding to the ligand binding domain (LBD) of AR. JJ-450 inhibits the transcriptional activity of AR and its splice variants (such as ARF876L) by inhibiting AR nuclear translocation and promoting the degradation of unliganded AR in the nucleus. JJ-450 can be used in castration-resistant prostate cancer (CRPC) studies that are resistant to Enzalutamide (MDV3100) (HY-70003).
    JJ-450
  • HY-P4786
    Acetyl-ACTH (7-24) (human, bovine, rat)
    Acetyl-ACTH (7-24) (human, bovine, rat) causes a marked decrease of ACTH-evoked corticosterone and aldosterone release.
    Acetyl-ACTH (7-24) (human, bovine, rat)
  • HY-W766769
    Cyproterone Acetate-13C2,d3
    		Antagonist
    Cyproterone Acetate-13C2,d3 is 13C-labeled Cyproterone Acetate (HY-13604).
    Cyproterone Acetate-<sup>13</sup>C<sub>2</sub>,d<sub>3</sub>
  • HY-160777B
    VNPP433-3β hydrochloride
    		Degrader
    VNPP433-3β (Galeterone 3β-imidazole) hydrochloride 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 hydrochloride induces cell apoptosis. VNPP433-3β hydrochloride inhibits tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β hydrochloride can be used for the study of castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC).
    VNPP433-3β hydrochloride
  • HY-153772
    Androgen receptor antagonist 8
    		Antagonist
    Androgen receptor antagonist 8 (Example 13) is an androgen receptor antagonist. Androgen receptor antagonist 8 inhibits prostate specific antigen secretion in LNcap cell (IC50: 88 nM). Androgen receptor antagonist 8 can be used for prostate cancer research.
    Androgen receptor antagonist 8
  • HY-159739
    M17-B15
    		Inhibitor
    M17-B15 is an androgen receptor dimerization inhibitor with an IC50 of 30 nM. M17-B15 effectively disrupts AR self-association, thereby suppressing AR signaling. M17-B15 exhibits extraordinary anti- prostate cancer (PCa) efficacy in vitro and in mouse xenograft tumor models.M17-B15 can be used for the study of prostate cancer.
    M17-B15
  • HY-P11642
    Sialorphin
    Sialorphin is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin is also a copper (II) ion-binding ligand. Sialorphin has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease.
    Sialorphin
  • HY-178148
    AR antagonist 17
    		Antagonist
    AR antagonist 17 is a selective, orally active, low brain-penetrant Androgen Receptor (AR) antagonist (IC50 = 0.010 μM), effectively blocking AR dimerization and nuclear translocation, and demonstrating potent efficacy in several castration-resistant prostate cancer (CRPC) cells. AR antagonist 17 showed superior efficacy against variant drug-resistant AR mutants. AR antagonist 17 can inhibit tumor growth in an LNCaP xenograft model without apparent toxicity. AR antagonist 17 can be used for the study of castration-resistant prostate cancer (CRPC).
    AR antagonist 17
  • HY-173474
    ERβ agonist-1
    		Antagonist
    ERβ agonist-1 (Compound 8) is a dual-active selective ERβ agonist (EC50: 46.8 nM) and AR antagonist (IC50: 1555 nM). ERβ agonist-1 activates ERβ signaling by binding to ERβ and inhibits AR activity. ERβ agonist-1 retains selective ERβ agonist activity in mouse models and can be used to study prostate cancer.
    ERβ agonist-1
  • HY-173409
    AR antagonist 11
    		Antagonist
    AR antagonist 11 (Compound c2) is a selective AR antagonist with an IC50 of 0.019 μM. AR antagonist 11 is also effective against ARF877L/T878A mutant (IC50: 1.03 μM). AR antagonist 11 inhibits LNCaP cell proliferation and reduces PSA protein expression (IC50: 0.54 μM). AR antagonist 11 can be used for research of prostate cancer (PCa).
    AR antagonist 11
  • HY-19337S
    Ketodarolutamide-d3
    		Antagonist
    Ketodarolutamide-d3 (BAY 1896953-d3) is the deuterium labeled Ketodarolutamide (HY-19337). Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a Ki value of 8 nM for rat wild-type AR and an IC50 value of 38 nM in AR-HEK293 cells. Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs. Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer.
    Ketodarolutamide-d<sub>3</sub>
  • HY-162764
    Androgen receptor degrader-5
    		Degrader
    Androgen receptor degrader-5 (compound 14k) exhibits promising properties, including superior androgen receptor degradation activity and antiproliferative activity.
    Androgen receptor degrader-5
  • HY-146026
    Androgen receptor antagonist 3
    		Antagonist
    Androgen receptor antagonist 3 (Compound C18) is an androgen receptor (AR) antagonist with an IC50 of 2.4 μM. Androgen receptor antagonist 3 shows anticancer activities.
    Androgen receptor antagonist 3
  • HY-139970
    VPC-13789
    		Inhibitor
    VPC-13789 is a potent, selective, and orally bioavailable antiandrogen. VPC-13789 can be used for the research of castration-resistant prostate cancer (CRPC) therapeutics. VPC-13789 inhibits androgen receptor (AR) transcriptional activity in LNCaP cells (IC50=0.19 μM).
    VPC-13789
  • HY-176067
    LO-4-25
    		Degrader
    LO-4-25 is a covalent degrader targeting the androgen receptor (AR) and its truncated variant AR-V7. LO-4-25 covalently binds to the E3 ubiquitin ligase CUL4 DCAF16, promoting the ubiquitination of AR and AR-V7, which subsequently are recognized and degraded by the proteasome, reducing the protein levels of AR and AR-V7 in cells. LO-4-25 is promising for research of androgen-independent prostate cancers.
    LO-4-25
  • HY-150878
    AR ligand-4
    		Ligand
    AR ligand-4 is an androgen receptor (AR) ligand, which can be used for the synthesis of PROTACs, such as ARD-1676 (HY-156111).
    AR ligand-4
  • HY-175456
    AR-DBD ligand-1
    AR-DBD ligand-1 is an AR-DBD ligand. AR-DBD ligand-1 can be used to synthesize PROTAC LYA914 (HY-175455).
    AR-DBD ligand-1
  • HY-N15686
    Torulene
    		Inhibitor
    Torulene (Torulin) is an orally active carotenoid with anti-cancer activity. Torulene inhibits proliferation and induces apoptosis of tumor cells via a mitochondrial signal pathway and the down-regulation of androgen receptor (AR) expression. Torulene can be used for the study of prostate cancer.
    Torulene
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity