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-B0022R
    Flutamide (Standard)
    		Antagonist
    Flutamide (Standard) is the analytical standard of Flutamide. This product is intended for research and analytical applications. Flutamide is an Androgen Receptor antagonist with Ki=55 nM. Flutamide inhibits prostate cancer progression and has synergistic effects with Docetaxel (HY-B0011). Flutamide also has the potential to protect against hyperthermia-induced multiple organ dysfunction syndrome.
    Flutamide (Standard)
  • HY-W011927R
    4,4'-Sulfonyldiphenol (Standard)
    		Inhibitor
    4,4'-Sulfonyldiphenol (Bisphenol S; Bis(4-hydroxyphenyl) sulfone) (Standard) is the analytical standard of 4,4'-Sulfonyldiphenol (HY-W011927). This product is intended for research and analytical applications. 4,4'-Sulfonyldiphenol, a substitute for Bisphenol A (HY-18260), is widely used in industrial and consumer products. 4,4'-Sulfonyldiphenol is an estrogen receptor (ER) agonist and can competitively bind to thyroid hormone receptors (TR) with IC50 values for TRα and TRβ are 2650 μM and 2294 μM respectively, thereby affecting breast development and reducing the expression of androgen receptor (AR) in fetal testes. 4,4'-Sulfonyldiphenol promotes the progression of glioblastoma by upregulating the EZH2 mediated PI3K/AKT/mTOR pathway. Under chronic exposure, 4,4'-Sulfonyldiphenol can cause significant lipid deposition and dyslipidemia in the mouse liver by upregulating JunB and Atf3, and has a role in causing obesity at low doses. 4,4'-Sulfonyldiphenol induces intestinal inflammation by altering the intestinal microbiome. 4,4'-Sulfonyldiphenol accelerates the progression of atherosclerosis in zebrafish embryo larvae.
    4,4'-Sulfonyldiphenol (Standard)
  • HY-16060S2
    Apalutamide-13C,d3
    		Antagonist 99.90%
    Apalutamide-13C,d3 is the 13C- and deuterium labeled Apalutamide. Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM.
    Apalutamide-<sup>13</sup>C,d<sub>3</sub>
  • HY-U00229
    Bifluranol
    		Inhibitor 98.88%
    Bifluranol (BX341) is an anti-androgen.
    Bifluranol
  • HY-45509
    TLB 150 Benzoate
    		Modulator 98.3%
    TLB 150 Benzoate (RAD150) is the modulator for androgen receptor with an IC50 of 0.13 μM.
    TLB 150 Benzoate
  • HY-16985R
    Darolutamide (Standard)
    		Antagonist
    Darolutamide (Standard) is the analytical standard of Darolutamide. This product is intended for research and analytical applications. Darolutamide (ODM-201;BAY-1841788) is a potent androgen receptor (AR) antagonist with an IC50 of 26 nM in in vitro assay.
    Darolutamide (Standard)
  • HY-N2908R
    Atraric acid (Standard)
    		Antagonist
    Atraric acid (Standard) is the analytical standard of Atraric acid. This product is intended for research and analytical applications. Atraric acid (Methyl atrarate) is a specific androgen receptor (AR) antagonist with anti-inflammatory and anticancer effects. Atraric acid represses the expression of the endogenous prostate specific antigen gene in both LNCaP and C4-2 cells. Atraric acid can also inhibit the synthesis of NO and cytokine, and suppress the MAPK-NFκB signaling pathway. Atraric acid can be used to research prostate diseases and inflammatory diseases[1][2].
    Atraric acid (Standard)
  • HY-115282
    JNJ-63576253 free base
    		Antagonist
    JNJ-63576253 (TRC-253) free base is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 free base can be used for the research of castration-resistant prostate cancer (CRPC).
    JNJ-63576253 free base
  • HY-157491
    K2-B4-5e
    		Degrader
    K2-B4-5e is a E3 ligase KLHDC2-based BRD4 and androgen receptor (AR) degradation PROTAC. K2-B4-5e is capable of inducing rapid and robust degradation of BET-family and AR proteins in cells.
    K2-B4-5e
  • HY-159844
    Gridegalutamide
    Gridegalutamide has antiandrogen and antitumor activities.
    Gridegalutamide
  • HY-111421
    ODM-204
    		Inhibitor
    ODM-204 is novel nonsteroidal dual inhibitor of both androgen receptor and CYP17A1 enzyme, with IC50s of 80 nM and 22 nM, respectively.
    ODM-204
  • HY-13702S
    Nilutamide-d6
    		Antagonist 99.77%
    Nilutamide-d6 (Nilandron-d6) is the deuterium labeled Nilutamide. Nilutamide (Nilandron) is a non-steroidal anti-androgen agent proposed in the research of metastatic prostatic carcinoma.
    Nilutamide-d<sub>6</sub>
  • HY-162423
    CYB210010
    		Agonist
    CYB210010 is an orally bioavailable, long-acting serotonin 5-HT2 receptor agonist that selectively targets 5-HT2A and 5-HT2C receptors (EC50: 4.1 n, 7.3 nM). CYB210010 can enter the central nervous system, cause a head twitch response (HTR), and is not prone to behavioral tolerance during chronic administration.
    CYB210010
  • HY-14249S
    Bicalutamide-d4
    		Antagonist
    Bicalutamide-d4 is the deuterium labeled Bicalutamide. Bicalutamide is an orally active non-steroidal androgen receptor (AR) antagonist. Bicalutamide can be used for the research of prostate cancer.
    Bicalutamide-d<sub>4</sub>
  • HY-403733B
    (+)-JJ-450
    		Antagonist
    (+)-JJ-450 is a non-competitive antagonist targeting the androgen receptor (AR) that inhibits AR nuclear localization and transcriptional activity in the absence of androgen. (+)-JJ-450 is less active than (-)-JJ-450 (HY-403733A) in inhibiting prostate-specific antigen (PSA) expression in LN95 cells, possibly because (+)-JJ-450 targets the ligand binding domain (LBD) of AR. (+)-JJ-450 inhibits the transcriptional activity of AR and its splice variants (e.g., ARv7) by promoting the degradation of unliganded AR in the nucleus and reducing the binding of AR to androgen response elements (AREs). (+)-JJ-450 can be used in castration-resistant prostate cancer (CRPC) studies that are resistant to enzalutamide (MDV3100) (HY-70003).
    (+)-JJ-450
  • HY-113233
    19-Noretiocholanolone
    19-Noretiocholanolone is an anabolic androgenic steroid metabolite of Nandrolone.
    19-Noretiocholanolone
  • 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.
    ID11916
  • HY-135473
    Chlormadinone
    		Inhibitor
    Chlormadinone is an antiandrogen agent. Chlormadinone can be used for the study of benign prostatic hyperplasia (BPH).
    Chlormadinone
  • HY-W411296
    6α-Chloro testosterone
    6α-Chloro testosterone is an anabolic androgenic steroid.
    6α-Chloro testosterone
  • 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.
    SHBG(141–161)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity