1. Signaling Pathways
  2. Vitamin D Related/Nuclear Receptor
  3. Androgen Receptor
  4. Androgen Receptor Inhibitor

Androgen Receptor Inhibitor

Androgen Receptor Inhibitors (39):

Cat. No. Product Name Effect Purity
  • HY-138641
    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.
  • HY-111848A
    PROTAC AR Degrader-4 TFA
    Inhibitor ≥98.0%
    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).
  • HY-N0790
    Inhibitor ≥98.0%
    Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent androgen receptor (AR) inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC).
  • HY-130492
    Inhibitor 99.54%
    ARCC-4 is a low-nanomolar Androgen Receptor (AR) degrader based on PROTAC, with a DC50 of 5 nM. ARCC-4 is an enzalutamide-based von Hippel-Lindau (VHL)-recruiting AR PROTAC and outperforms enzalutamide. ARCC-4 effectively degrades clinically relevant AR mutants associated with antiandrogen therapy.
  • HY-N1943
    Inhibitor 99.76%
    Ailanthone (Δ13-Dehydrochaparrinone) is a potent inhibitor of both full-length androgen receptor (AR) (IC50=69 nM) and constitutively active truncated AR splice variants (AR1-651 IC50=309 nM).
  • HY-16079
    Inhibitor 99.32%
    AZD3514 is an orally activie and selective androgen receptor (AR) inhibitor. AZD3514 androgen-dependently and -independently inhibits AR signal. AZD351 down-regulates nuclear AR levels in human LNCaP prostate cancer cells in the absence of androgen with an pIC50 value of 5.75. AZD3514 can be used for the research of prostate cancer.
  • HY-15194
    Inhibitor 98.06%
    Dimethylcurcumin (ASC-J9) is an androgen receptor degradation enhancer that effectively suppresses castration resistant prostate cancer cell proliferation and invasion.
  • HY-100348
    Inhibitor 98.87%
    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.
  • HY-116501
    Inhibitor 98.89%
    VPC-14449 is a potent and selective inhibitor of the DNA-binding domain of the androgen receptor (AR-DBD), with IC50 of 0.34 μM for full-length human AR. VPC-14449 reduces the ability of full-length AR as well as AR variants to interact with chromatin. VPC-14449 can be used for the research of prostate cancer.
  • HY-11027
    Inhibitor 98.39%
    MK-0773 is a selective androgen receptor modulators (SARMs) that binds to AR with an IC50 of 6.6 nM.
  • HY-133020
    Inhibitor 99.67%
    ARD-266 is a highly potent and von Hippel-Lindau E3 ligase-based Androgen Receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM.
  • HY-139436
    Inhibitor 99.48%
    ARD-2585 is an exceptionally potent and orally active PROTAC degrader of androgen receptor.
  • HY-123875A
    Ralaniten triacetate
    Inhibitor 98.79%
    Ralaniten triacetate (EPI-506), the pro-drug of Ralaniten, is a first-in-class, orally active androgen receptor (AR) N-terminal domain (NTD) inhibitor. Ralaniten triacetate shows activity against both full length and resistance-related AR species, including AR-v7.
  • HY-141487
    CLP-3094 is a potent BF3 (binding function 3)-directed inhibitor of the androgen receptor (AR). CLP-3094 inhibits AR transcriptional activity (IC50=4 μM). CLP-3094 is a selective, potent GPR142 antagonist.
  • HY-19319
    Inhibitor 99.71%
    MI-136 is an inhibitor of the menin-MLL protein-protein interaction (PPI), with an IC50 of 31 nM and a Kd of 23.6 nM. MI-136 shows to block AR signaling and has the potential for the study in castration-resistant tumors.
  • HY-145479
    PROTAC AR-V7 degrader-1
    Inhibitor 99.34%
    PROTAC AR-V7 degrader-1 (Compound 6) is a potent, orally bioavailable and selective AR-V7 degrader with the DC50 of 0.32 µM by recruiting VHL E3 ligase to Androgen receptor (AR) DNA binding domain (DBD) binder. PROTAC AR-V7 degrader-1 exhibits activity against 22Rv1 cell-line expressing AR-V7 with the EC50 of 0.88 µM.
  • HY-132292
    Inhibitor 99.40%
    ARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer.
  • HY-124292
    Honokiol DCA
    Honokiol DCA (Honokiol dichloroacetate) is a dichloroacetate analog of Honokiol. Honokiol DCA can inhibit the growth of human prostate cancer cells in vitro and suppress the androgen receptor (AR) protein level.
  • HY-112895A
    Inhibitor 98.35%
    (R)-UT-155 (compound 11) is a selective androgen receptor degrader (SARD) ligand. Less active than the S-isomer.
  • HY-110028
    Leelamine hydrochloride
    Inhibitor 98.10%
    Leelamine hydrochloride is a tricyclic diterpene molecule that is extracted from the bark of pine trees. Leelamine hydrochloride is a cannabinoid receptor type 1 (CB1) agonist and a inhibitor of SREBP1-regulated fatty acid/lipid synthesis in prostate cancer cells that is not affected by androgen receptor status. Leelamine hydrochloride suppresses transcriptional activity of androgen receptor, which is known to regulate fatty acid synthesis[2,3].