Home Endocrinology & Hormones Androgen Receptor

Androgen Receptor inhibitors/antagonist

After binding to androgenic hormones such as testosterone and dihydrotestosterone, the androgen receptor (AR, NR3C4, nuclear receptor subfamily 3, group C, member 4) as a nuclear receptor can be activated and then translocate into nucleus. Activated AR can interact with caveolae resultling in the activation of Erk, PI3K, SRC and Akt signaling pathways. Growth factors such as insulin-like growth-factor-1 (IGF-1), keratinocyte growth factor (KGF) and epidermal growth factor (EGF), and receptor-tyrosine kinases (RTKs) such as HER-2/neu can activate AR independently of androgens via mitogen activated protein kinases (MAPK) and Akt pathways. RTKs and G-protein coupled receptors (GPCRs) are also found concentrated in caveolae, where AR may have roles in activation of these receptors. GPCRs can also phosphorylate AR independently of androgen via MEK1/2 and ERK1/2.

Other Endocrinology & Hormones Related Inhibitors

Adrenergic Receptor Estrogen/progestogen Receptor Aromatase 5-alpha Reductase RAAS Glucocorticoid Receptor ACE Mineralocorticoid Receptor PGDS Progesterone Receptor
Cat.No. Product Name Information Product Use Citations Product Validations
S1250 MDV3100 (Enzalutamide) Enzalutamide is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy.
Cancer Cell, 2025, 43(5):891-904.e10
Nat Genet, 2025, 57(10):2468-2481
Nat Genet, 2025, 57(12):3027-3038
Verified customer review of MDV3100 (Enzalutamide)
S1190 Bicalutamide Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. This compound promotes autophagy.
Nat Commun, 2025, 16(1):6587
Nat Commun, 2025, 16(1):6451
J Control Release, 2025, 380:417-432
Verified customer review of Bicalutamide
S7559 ODM-201 (Darolutamide) Darolutamide (ODM-201, BAY-1841788) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with Ki of 11 nM. Phase 3.
Nat Commun, 2025, 16(1):6587
Clin Cancer Res, 2025, 10.1158/1078-0432.CCR-24-1812
Cell Rep, 2025, 44(6):115779
Verified customer review of ODM-201 (Darolutamide)
S6965 Bavdegalutamide (ARV-110) Bavdegalutamide (ARV-110) is an orally bioavailable, specific androgen receptor (AR) PROTAC degrader that leads to ubiquitination and degradation of AR. This compound completely degrades androgen receptor (AR) in all cell lines tested with DC50 of < 1 nM, and can be used for the research of prostate cancer.
BMC Biol, 2025, 23(1):51
Cell Mol Life Sci, 2024, 81(1):324
Nucleic Acids Res, 2023, gkad642
S5285 RU58841 RU58841, also known as PSK-3841 or HMR-3841, is a non-steroidal anti-androgen.
S9667 Inobrodib (CCS-1477) Inobrodib (CCS1477; CBP-IN-1; CBP/p300-IN-4）is a potent and selective inhibitor of p300/CBP bromodomain. CCS1477 works by inhibiting the expression and function of the androgen receptor (AR), as well as inhibiting c-Myc.
Nat Genet, 2025, 57(10):2468-2481
Nat Commun, 2025, 16(1):4133
PLoS Pathog, 2025, 21(9):e1013073
E1573 Luxdegalutamide (ARV-766) Luxdegalutamide (ARV-766) is an orally active and potent degrader of proteolysis targeting chimera (PROTAC) protein. ARV-766 degrades wild-type androgen receptor (AR) but also relevant AR LBD mutants, including the most prevalent AR L702H, H875Y, and T878A mutations.
S2840 Apalutamide (ARN-509) Apalutamide (ARN-509) is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM in a cell-free assay. This compound is useful for prostate cancer treatment and is in Phase 3.
Nat Genet, 2025, 57(12):3027-3038
Nat Commun, 2025, 16(1):6587
J Control Release, 2025, 380:417-432
Verified customer review of Apalutamide (ARN-509)
S1908 Flutamide Flutamide (SCH-13521) is an antiandrogen drug, with its active metablolite binding at androgen receptor with Ki values of 55 nM, and this compound is primarily used to treat prostate cancer.
iScience, 2024, 27(10):110862
Zool Res, 2024, 45(2):355-366
Dis Model Mech, 2024, 17(10)dmm050900
Verified customer review of Flutamide
S4054 Spironolactone Spironolactone is a potent antagonist of the androgen receptor with IC50 of 77 nM.
Cancer Cell, 2025, 43(4):776-796.e14
J Clin Invest, 2025, 135(16)e187663
Biomed Pharmacother, 2024, 180:117523
Verified customer review of Spironolactone

Signaling Pathway Map