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-109619
    D4-abiraterone
    Antagonist 99.75%
    D4-abiraterone is a major metabolite of abiraterone. D4-abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor.
    D4-abiraterone
  • HY-160777
    VNPP433-3β
    Degrader 98.01%
    VNPP433-3β is a 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 inhibits proliferation of cancer cell LNCaP, C4-2B and CWR22Rv1 with GI50 of 0.2, 0.3 and 0.31 μM. VNPP433-3β exhibits good pharmacokinetic characters in CD-1 mouse and inhibits tumor growth in the CWR22Rv1 xenograft mouse model.
    VNPP433-3β
  • HY-103245
    Cl-4AS-1
    Agonist 99.64%
    Cl-4AS-1, a potent steroidal androgen receptor (AR) agonist (IC50 = 12 nM), is also an inhibitor of 5α-reductase types I and II (IC50 = 6 and 10 nM, respectively).
    Cl-4AS-1
  • HY-141487
    CLP-3094
    Inhibitor
    CLP-3094 is a potent BF3 (binding function 3)-directed inhibitor of the androgen receptor (AR). CLP-3094 inhibits AR transcriptional activity (IC50=4 μM). CLP-3094 is a selective, potent GPR142 antagonist.
    CLP-3094
  • HY-130845A
    AR antagonist 1 hydrochloride
    Antagonist 99.53%
    AR antagonist 1 (compound 29) hydrochloride is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020).
    AR antagonist 1 hydrochloride
  • HY-B0561R
    Spironolactone (Standard)
    Antagonist 98.55%
    Spironolactone (Standard) is the analytical standard of Spironolactone. This product is intended for research and analytical applications. 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.
    Spironolactone (Standard)
  • HY-149862
    ARD-2051
    98.19%
    ARD-2051 is a potent and orally active androgen receptor (AR) proteolysis-targeting chimera degrader. ARD-2051 achieves DC50 values of 0.6 nM for AR protein degradation in both the LNCaP and VCaP prostate cancer cell lines. ARD-2051 can be used for the research of prostate cancer.
    ARD-2051
  • HY-16060S
    Apalutamide-d4
    Antagonist 99.90%
    Apalutamide-d4 is a deuterium labeled Apalutamide. Apalutamide is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM[1].
    Apalutamide-d<sub>4</sub>
  • HY-B1866
    Linuron
    Antagonist 99.88%
    Linuron is a phenylurea herbicide that is widely used to control the growth of grass and weeds in various agriculture crops and in orchards. Linuron is a photosystem II inhibitor. Linuron is also a competitive androgen receptor (AR) antagonist with a Ki of 100 μM. Linuron shows reproductive toxicity in animals that acts as an endocrine disruptor.
    Linuron
  • HY-135732
    SK33
    Antagonist 99.98%
    SK33, a trifluoromethylated enobosarm analog, is a potent, and tissue selective anti-androgen. SK33reduces androgen receptor (AR) transcriptional activity.
    SK33
  • HY-N7045
    Isosilybin B
    Inhibitor 99.32%
    Isosilybin B is a flavonolignan. Isosilybin B can be isolated from Silybum marianum. Isosilybin B can regulate cell cycle-related proteins (e.g., reduce cyclins (D3, D1, A, E), Cdk4, Cdk2, Cdc25A), and activate Caspases (Caspase-9 and Caspase-3). Isosilybin B can promote Apoptosis, reduce androgen receptor (AR) and PSA. Isosilybin B has anticancer activity against prostate cancer.
    Isosilybin B
  • HY-B1986
    p,p'-DDE
    Antagonist 99.51%
    p,p'-DDE (4,4'-DDE) is the major and persistent metabolite of DDT. p,p'-DDE is a orally active androgen receptor antagonist with an IC50 of 5 μM and a Ki of 3.5 μM. p,p'-DDE can affect the development and function of the male reproductive system. Additionally, high serum concentrations of p,p'-DDE may be a risk factor for type 2 diabetes in women.
    p,p'-DDE
  • HY-161741
    VinclozolinM2-2204
    Degrader 98.00%
    VinclozolinM2-2204 is a androgen receptor (AR) AUTOTAC degrader, with an DC50 of 200 nM in LNCaP prostate cancer cells. VinclozolinM2-2204 induces the formation of AR+LC3+ autophagic membranes. VinclozolinM2-2204 can be used for the research of cancer.(Pink: AR inhibitor (HY-168296); Black: linker (HY-128833); Blue: CRBN Ligand (HY-168293))
    VinclozolinM2-2204
  • HY-160020
    ET516
    Inhibitor 99.13%
    ET516 is a potent inhibitor of Androgen Receptor. ET516 significantly inhibits the proliferation and tumor growth of prostate cancer cells expressing AR-resistant mutants.
    ET516
  • HY-14250
    PF-998425
    Antagonist 98.31%
    PF-998425 is a potent, selective nonsteroidal androgen receptor (AR) antagonist with an IC50 of 37 nM and 43 nM in AR binding and cellular assays, respectively. PF-998425 has low activity on common receptors and enzymes, such as progesterone receptor. PF-998425 can be used for sebum control and androgenetic alopecia research.
    PF-998425
  • HY-135794S
    11-Ketodihydrotestosterone-d3
    Agonist 99.00%
    11-Ketodihydrotestosterone-d3 is the deuterium labeled 11-Ketodihydrotestosterone. 11-Ketodihydrotestosterone (11-KDHT; 5α-Dihydro-11-keto testosterone) is an endogenous steroid and a metabolite of 11β-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a potent androgen receptor (AR) agonist with a Ki of 20.4 nM and an EC50 of 1.35 nM for human AR. 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostate cancer cells[1][2].
    11-Ketodihydrotestosterone-d<sub>3</sub>
  • HY-B0469S
    Medroxyprogesterone acetate-d3
    98.13%
    Medroxyprogesterone acetate-d3 is deuterium labeled Medroxyprogesterone acetate. Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors[1].
    Medroxyprogesterone acetate-d<sub>3</sub>
  • HY-163340
    GA32
    Inhibitor 99.67%
    GA32 (compound 58r) is potent androgen receptor (AR)/glucocorticoid receptor (GR) dual inhibitor with IC50 values of 0.13 μM and 0.83 μM for AR and GR, respectively. GA32 inhibits the proliferation of Enzalutamide (HY-70002) resistance castration-resistant prostate cancer both in vitro and in vivo.
    GA32
  • HY-103246
    TFM-4AS-1
    99.96%
    TFM-4AS-1 is a selective androgen receptor modulator (SARM), and a potent androgen receptor (AR) ligand with an IC50 of 38 nM. TFM-4AS-1 is a gene-selective agonist.
    TFM-4AS-1
  • HY-B0561S1
    Spironolactone-d3
    Antagonist 99.82%
    Spironolactone-d3 is the 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>
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity