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-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-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-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-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-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
  • HY-N0475R
    Triptophenolide (Standard)
    		Antagonist
    Triptophenolide (Standard) is the analytical standard of Triptophenolide. This product is intended for research and analytical applications.
    Triptophenolide (Standard)
  • HY-173626
    EN1441
    		Degrader
    EN1441 is a covalent degrader targeting the androgen receptor (AR) with an EC50 value of 4.2 μM and its truncated variant AR-V7. EN1441 selectively and potently degrades both AR and AR-V7 in androgen-independent prostate cancer cells. EN1441 is promising for research of androgen-independent prostate cancers.
    EN1441
  • HY-155666
    YXG-158
    		Degrader
    YXG-158 (Compound 23-h) is an orally active AR degrader and CYP17A1 inhibitor. YXG-158 has AR degradation activity with DC50 value of 1.28 μM. YXG-158 can inhibit CYP17A1 with IC50 value of 100 nM. XG-158 can be used for the research of enzalutamide-resistant prostate cancer.
    YXG-158
  • HY-170330
    AR ligand-33
    		Ligand
    AR ligand-33 is the ligand for androgen receptor, that can be used for synthesis of PROTAC AR Degrader-8 (HY-170329) as the target protein ligand.
    AR ligand-33
  • HY-170450
    AR ligand-38
    		Ligand
    AR ligand-38 is the ligand for androgen receptor, that can be used for synthesis of PROTAC AR Degrader-9 (HY-170448).
    AR ligand-38
  • HY-151266
    AR antagonist 4
    		Antagonist
    AR antagonist 4 (Compound 67-b) is an orally active androgen receptor (AR) antagonist with an IC50 of 246.6 nM against wt-AR, and is also an AR degrader with a DC50 of 2.84 μM.
    AR antagonist 4
  • HY-160221
    PROTAC AR Degrader-7
    PROTAC AR Degrader-7 (compound 99) is a PROTAC targeting androgen receptor with an IC50 value of 3 nM. PROTAC AR Degrader-7 is composed of PROTAC target protein ligand AR ligand-32 (HY-170303) (red part), E3 ligase ligand E3 ligase Ligand 44 (HY-170304) (blue part) and PROTAC Linker N-Boc-piperazine (HY-30105) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is E3 Ligase Ligand-linker Conjugate 145 (HY-170305).
    PROTAC AR Degrader-7
  • HY-103578
    S-40503
    		Modulator
    S-40503 is an orally active and selective androgen receptor modulator. S-40503 significantly increases the bone mineral density (BMD) and biomechanical strength of femoral cortical bone.
    S-40503
  • HY-138151
    3'-Hydroxy stanozolol
    		Control
    3'-Hydroxy stanozolol is a major metabolite of the anabolic androgenic steroid Stanozolol.
    3'-Hydroxy stanozolol
  • HY-14249S1
    Bicalutamide-d5
    		Antagonist
    Bicalutamide-d5 is deuterated labeled Bicalutamide (HY-14249). Bicalutamide is an orally active non-steroidal androgen receptor (AR) antagonist. Bicalutamide can be used for the research of prostate cancer.
    Bicalutamide-d<sub>5</sub>
  • HY-163510
    AR/AR-V7-IN-1
    		Inhibitor
    AR/AR-V7-IN-1 (Compound 20i) is an AR/ARV7 inhibitor (IC50 = 172.85 nM). AR/AR-V7-IN-1 potently inhibits cell growth with IC50 values of 4.87 and 2.07 μM in the LNCaP and 22RV1 cell lines, respectively. AR/AR-V7-IN-1 exhibits effective tumor growth inhibition in the 22RV1 xenograft study. AR/AR-V7-IN-1 can be used for the research of prostate cancer.
    AR/AR-V7-IN-1
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity