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).

Androgen Receptor Related Products (322):

Cat. No. Product Name Effect Purity
  • HY-16985
    Darolutamide Antagonist 99.49%
    Darolutamide (ODM-201;BAY-1841788) is a potent androgen receptor (AR) antagonist with an IC50 of 26 nM in in vitro assay.
  • HY-70002
    Enzalutamide Antagonist
    Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells. Enzalutamide is an autophagy activator[1][2].
  • HY-138641
    Bavdegalutamide Inhibitor 99.64%
    Bavdegalutamide (ARV-110) is an orally active, specific androgen receptor (AR) PROTAC degrader. Bavdegalutamide promotes ubiquitination and degradation of AR. Bavdegalutamide can be used for the research of prostate cancer (Pink: AR ligand (HY-168299); Blue: E3 ligase ligand (HY-W093272); Black: linker (HY-W091986))[1].
  • HY-14650
    DHEA Inhibitor
    DHEA (Prasterone) is one of the most abundant steroid hormones. DHEA (Prasterone) mediates its action via multiple signaling pathways involving specific membrane receptors and via transformation into androgen and estrogen derivatives (e.g., androgens, estrogens, 7α and 7β DHEA, and 7α and 7β epiandrosterone derivatives) acting through their specific receptors.
  • HY-B0469
    Medroxyprogesterone acetate 99.88%
    Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors[1].
  • HY-172612
    AR antagonist 13 Antagonist
    AR antagonist 13 (compound 19) is an androgen receptor antagonist with inhibition rates exceeding 71.5% at 10 μM. AR antagonist 13 inhibits prostate cancer cell growth[1].
  • HY-176048
    ChEMBL22003 Modulator
    ChEMBL22003 is a potential phase separation modulator of ARV7 that can bind to the ARV7 binding sites. ChEMBL22003 has potential for use in the research of prostate cancer[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)[1].
  • HY-14249
    Bicalutamide Antagonist
    Bicalutamide is an orally active non-steroidal androgen receptor (AR) antagonist. Bicalutamide can be used for the research of prostate cancer[1].
  • HY-118409
    VPC-3033 Antagonist
    VPC-3033 is an androgen receptor antagonist. VPC-3033 has a strong androgen DHT replacement potency (IC50: 0.625-2.5 μM), can effectively inhibit androgen receptor transcriptional activity (IC50=0.3 μM), and has a strong androgen receptor degradation ability. In addition, VPC-3033 exhibits significant anti-androgen receptor activity against prostate cancer cells resistant to Enzalutamide (HY-70002)[1].
  • HY-113233
    19-Noretiocholanolone
    19-Noretiocholanolone is an anabolic androgenic steroid metabolite of Nandrolone[1].
  • HY-173640
    ID11916 Antagonist
    ID11916 is an orally active androgen receptor (AR) antagonist and a phosphodiesterase 5 (PDE5) inhibitor. ID11916 blocks androgen binding to AR, nuclear translocation, and androgen-dependent transcriptional activity of AR, while increasing intracellular cGMP levels and activating PKG via inhibition. ID11916 shows potent anti-cancer effect in prostate cancer cell lines VCaP and 22Rv1 and in AR-positive breast cancer cell lines SK-BR-3[1].
  • HY-100348
    EPI-001 Inhibitor 99.34%
    EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer[1][2][3].
  • HY-135473
    Chlormadinone Inhibitor
    Chlormadinone is an antiandrogen drug. Chlormadinone combined with Tamsulosin shows greater improvement in subjective symptoms of BPH[1].
  • HY-W411296
    6α-Chloro testosterone
    6α-Chloro testosterone is an anabolic androgenic steroid.
  • HY-111848A
    PROTAC AR Degrader-4 TFA Inhibitor 99.26%
    PROTAC AR Degrader-4 comprises a IAP ligand binding group, a linker and an Androgen Receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1].
  • HY-P10413
    SHBG(141–161) Agonist
    SHBG 141-161 is a GPRC6A receptor agonist. SHBG 141-161 mimics the action of GPRC6A endogenous agonist uncarboxylated osteocalcin by binding to GPRC6A and promoting downstream signaling to increase testosterone and insulin secretion. SHBG 141-161 also reduces the affinity of GPRC6A to GDP protein by binding to the outer cell domain of GPRC6A thus affecting the dynamics of signal transduction. SHBG 141-161 can be used to study GPRC6A in energy metabolism and endocrine regulation[1].
  • HY-B1986S
    p,p'-DDE-d8
    p,p'-DDE-d8 is the deuterium labeled p,p'-DDE[1]. p,p'-DDE (4,4'-DDE), a major metabolite of persistent dichlorodiphenyltrichloroethane (DDT), is a potent androgen receptor antagonist, with an IC50 of 5 μM and a Ki of 3.5 μM[2].
  • 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[1][2][3].
  • HY-120018
    VPC-13566 Inhibitor 99.87%
    VPC-13566, a BF3-specific small molecule, is an androgen receptor (AR) inhibitor. VPC-13566 is effective in inhibiting AR transcriptional activity in vitro as well as the growth of AR-dependent PCa cell lines. VPC-13566 can be used as a chemical probe to help identify unknown AR partners.VPC-13566 can be used for the research of cancer.