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-N7043R
    Isosilybin A (Standard)
    		Inhibitor
    Isosilybin A (Standard) is the analytical standard of Isosilybin A (HY-N7043). Isosilybin A is a PPARγ agonist that can be isolated from silymarin. Isosilybin A activates extrinsic and intrinsic pathways of apoptosis through targeting of the Akt-NF-kB-AR axis. Isosilybin A can relieve the inflammatory response in the rosacea model via inhibiting Erk and p38 signaling pathways and M1 macrophage polarization, with its targets related to RELA and VEGFA. Isosilybin A has anti-prostate cancer (PCA) activity[1][2][3].
    Isosilybin A (Standard)
  • HY-135473S
    Chlormadinone-d6
    		Inhibitor
    Chlormadinone-d6 is the deuterium labeled Chlormadinone (HY-135473) . Chlormadinone is an antiandrogen agent. Chlormadinone can be used for the study of benign prostatic hyperplasia (BPH).
    Chlormadinone-d<sub>6</sub>
  • HY-156751
    (Rac)-GDC-2992
    		Degrader
    (Rac)-GDC-2992 (Compound 1) is a PROTAC androgen receptor degrader (DC50: 10 nM in VCaP cell). (Rac)-GDC-2992 blocks the process of androgen receptor transduction and also degrades the receptor itself. (Rac)-GDC-2992 can be used for prostate cancer research. Pink: AR ligand (HY-130845); Blue: E3 ligase ligand (HY-W1003189); Black: linker (HY-169975).
    (Rac)-GDC-2992
  • HY-163813
    AR Degrader-2
    		Degrader
    AR Degrader-2 (Compound 2) is a molecular glue that degrades androgen receptor (AR) with a DC50 of 0.3-0.5 μM in cell VCaP.
    AR Degrader-2
  • HY-W013272R
    Hydroxyflutamide (Standard)
    		Antagonist
    Hydroxyflutamide (Standard) is the analytical standard of Hydroxyflutamide. This product is intended for research and analytical applications. Hydroxyflutamide (HF), an active metabolite of Flutamide, is a potent androgen receptor antagonist (IC50=700 nM). Hydroxyflutamide can be used for the research of prostate cancer.
    Hydroxyflutamide (Standard)
  • HY-176128
    BWA-6047
    		Degrader
    BWA-6047 is a dual AR/AR-V7 and GSPT1 PROTAC degrader (AR: DC50 = 3.7 nM; AR-V7: DC50 = 3.0 nM; GSPT1: DC50 = 1.2 nM). BWA-6047 promotes ubiquitination and degradation of AR/AR-V7 and, through its molecular glue properties, induces the formation of a PPI between GSPT1 and CRBN, leading to GSPT1 degradation. BWA-6047 can be used in prostate cancer research (Pink: AR/AR-V7 ligand (HY-176129); Blue: E3 CRBN ligand (HY-W069604); Black: linker (HY-W069604)).
    BWA-6047
  • HY-126464
    Estromustine
    		Modulator
    Estromustine (EoM) is the active metabolite of Estramustine phosphate (HY-13627A). Estromustine binds to mutant androgen receptor (m-AR) with EC50 of 2.6 μM in LNCaP, exhibits cytotoxicity in human prostate cells LNCaP with IC50 of 9.73 μM.
    Estromustine
  • 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.
    ChEMBL22003
  • HY-170448
    PROTAC AR Degrader-9
    		Degrader
    PROTAC AR Degrader-9 (Compound c6) is a PROTAC degrader for androgen receptor, that degrades AR in human hair follicle papilla cells (HDPCs) with a DC50 of 262.38 nM. PROTAC AR Degrader-9 promotes the expressions of paracrine factors, such as TGF-β1 and β-catenin, exhibits hair regenerating efficacy in mouse models. (Pink: ligand for target protein AR ligand-38 (HY-170450); Black: linker; Blue: ligand for E3 ligase Cereblon (HY-170449))
    PROTAC AR Degrader-9
  • HY-163641
    AR Degrader-1
    		Degrader
    AR Degrader-1 (Compound ML 2-9) is a molecular glue androgen receptor (AR) monovalent degrader. AR Degrader-1 degrades AR through DCAF16 (E3 ligase) without obvious cytotoxicity in LNCaP prostate cancer cells.
    AR Degrader-1
  • HY-174391
    AR antagonist 15
    		Inducer
    AR antagonist 15 is an orally active androgen receptor (AR) antagonist with the IC50 of 97 nM for ART787A. AR antagonist 15 disrupts AR nuclear translocation, hinders AR homodimerization, and suppresses transcription of AR-regulated genes by competitive binding to the ligand binding pocket. AR antagonist 15 can significantly lower the prostate-specific antigen (PSA) level. AR antagonist 15 induces apoptosis by reducing the expression of apoptosis pathway related proteins. AR antagonist 15 can be used for the research of prostate cancer.
    AR antagonist 15
  • HY-160262
    AR/BET protein degrader-1
    		Degrader
    AR/BET protein degrader-1 (Compound 149) is an Androgen Receptor and BET (bromodomain and extra-terminal domain) protein degrader that can be used in cancer research.
    AR/BET protein degrader-1
  • HY-172908
    Androgen receptor antagonist 13
    		Antagonist
    Androgen receptor antagonist 13 (compound 8a) is an orally active Androgen receptor antagonist with an IC50 of 0.20 μM. Androgen receptor antagonist 13 can be used in the study of prostate cancer.
    Androgen receptor antagonist 13
  • HY-N2345R
    Procyanidin B3 (Standard)
    		Inhibitor
    Procyanidin B3 (Standard) is the analytical standard of Procyanidin B3. This product is intended for research and analytical applications. Procyanidin B3 is a natural product with antioxidant activity and oral bioavailability, possessing good blood-brain barrier penetration. Procyanidin B3 is a selective inhibitor of histone acetyltransferase (HAT). By inhibiting p300 HAT-mediated acetylation of the androgen receptor (androgen receptor). Procyanidin B3 alleviates intervertebral disc degeneration (IVDD) by inhibiting the formation of the TLR4/MD-2 complex. Procyanidin B3 can be used in research on prostate cancer and arthritis.
    Procyanidin B3 (Standard)
  • HY-111024R
    2,2,5,7,8-Pentamethyl-6-Chromanol (Standard)
    		Modulator
    2,2,5,7,8-Pentamethyl-6-Chromanol (Standard) is the analytical standard of 2,2,5,7,8-Pentamethyl-6-Chromanol. This product is intended for research and analytical applications. 2,2,5,7,8-Pentamethyl-6-Chromanol (PMC) is the anti-oxidant moiety of vitamin E (α-tocopherol). 2,2,5,7,8-Pentamethyl-6-Chromanol has potent androgen receptor (AR) signaling modulation and anti-cancer activity against prostate cancer cell lines[1].
    2,2,5,7,8-Pentamethyl-6-Chromanol (Standard)
  • HY-163485
    AR antagonist 8
    		Inhibitor
    AR antagonist 8 (compound 16), an unnatural entestrane, is a potent Lupeol-inspired androgen receptor (AR) antagonist with an IC50 of 0.76 μM.
    AR antagonist 8
  • HY-B0022S
    Flutamide-d7
    		Antagonist
    Flutamide-d7 is deuterium labeled Flutamide.
    Flutamide-d<sub>7</sub>
  • HY-P11007
    β-catenin inhibitory peptoid
    		Inhibitor
    β-catenin inhibitory peptoid (compound 13) inhibits the β-catenin:TCF interaction with an IC50 of 5.44 µM. β-catenin inhibitory peptoid inhibits both Wnt (IC50 of 0.105 µM) and androgen receptor (AR)-signaling (IC50 of 1.02 µM) in prostate cancer cell lines. β-catenin inhibitory peptoid markedly diminishes cell proliferation of prostate cancer cell lines.
    β-catenin inhibitory peptoid
  • HY-403733A
    (–)-JJ-450
    		Antagonist
    (-)-JJ-450 is a non-competitive antagonist targeting the androgen receptor (AR). (-)-JJ-450 is more potent than (+)-JJ-450 (HY-403733B) in inhibiting androgen-induced AR activity, and the mechanism of AR inhibition by (+)-JJ-450 is different from that of Enzalutamide (MDV3100) (HY-70003), which may target the ligand binding domain (LBD) of AR. (-)-JJ-450 inhibits the transcriptional activity of wild-type AR and mutant ARF876L by inhibiting AR nuclear translocation and promoting nuclear degradation of unbound AR. (-)-JJ-450 can be used in the study of castration-resistant prostate cancer (CRPC) resistant to Enzalutamide.
    (–)-JJ-450
  • HY-149434
    PROTAC AR-NTD degrader 1
    PROTAC AR-NTD antagonist 1 (compound 18) is a small molecule protein-targeting chimera (PROTACs) targeting the Androgen Receptor AR-V7. PROTAC AR-NTD antagonist 1 antagonizes the N-terminal domain of AR (AR-NTD), degrades AR-V7 protein, and induces apoptosis in prostate cancer (PC) cells. The efficiencies of PROTAC AR-NTD antagonist 1 in degrading AR-V7 in VCaP cells were 62.2% (1 μM) and 71.1% (5 μM), respectively.
    PROTAC AR-NTD degrader 1
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity