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-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-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
  • HY-146397
    TD-802
    		Inhibitor
    TD-802 (Compound 33c) is an androgen receptor (AR) PROTAC degrader with good microsomal stability. TD-802 has good antitumor efficacy in vivo and can be used for metastatic castration-resistant prostate cancer research.
    TD-802
  • HY-152520
    RLA-5331
    		Activator
    RLA-5331 is an iron activator containing anti-androgen. RLA-5331 has anti-proliferative activity on metastatic castration-resistant prostate cancer (mCRPC) cell line.
    RLA-5331
  • HY-171049
    Androgen receptor modulator 3
    		Modulator
    Androgen receptor modulator 3 is a selective modulator for androgen receptor that can be used for research of sarcopenia.
    Androgen receptor modulator 3
  • HY-B0561S2
    Spironolactone-d3-1
    		Antagonist
    Spironolactone-d3-1 is 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.
    Spironolactone-d<sub>3</sub>-1
  • HY-19470R
    Topilutamide (Standard)
    		Inhibitor
    Topilutamide (Standard) is the analytical standard of Topilutamide. This product is intended for research and analytical applications. Topilutamide is a topical nonsteroidal antiandrogen (NSAA).
    Topilutamide (Standard)
  • HY-13604S
    Cyproterone acetate-d3
    		Antagonist
    Cyproterone acetate-d3 is deuterium labeled Cyproterone acetate. Cyproterone acetate is an anti-androgen (IC50=7.1 nM) and progestogen synthetic steroid. Cyproterone acetate has affinity with progesteron and with glucocorticoidal receptors.
    Cyproterone acetate-d<sub>3</sub>
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity