Androgen Receptor

Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist (IC50=36 nM in LNCaP) that activates autophagy, exhibits antitumor activity, and is commonly used in treating desmoplasia-resistant prostate cancer.

Luxdegalutamide (ARV-766) is a novel, potent, and orally bioavailable proteolytic targeting chimera (PROTAC) protein degrader that degrades not only wild-type AR but also clinically relevant AR LBD mutants, including the most prevalent AR L702H, H875Y, and T878A mutations.

Topilutamide (Fluridil) is a topical nonsteroidal antiandrogen.

Bavdegalutamide (ARV-110) is an oral protein degrader that specifically binds to AR and mediates its degradation. Bavdegalutamide can degrade clinically relevant mutant AR proteins, maintain activity in a high androgen environment, and has an acceptable safety profile.

MK-3984 is a selective androgen receptor modulator, used in the study of conditions caused by androgen deficiency.

Masofaniten (EPI-7386) is an orally active androgen receptor (AR) inhibitor with antitumor activity for the study of prostate and breast cancers.

BMS-641988 is a novel nonsteroidal androgen receptor antagonist for the treatment of prostate cancer.

Rosolutamide (ALZ-003) is a curcumin analog, an orally active Nrf1 and Nrf2 activator.Rosolutamide modulates oxidative homeostasis, improves mitochondrial function and promotes autophagy, reduces mutant protein aggregation, and decreases intracellular/mitochondrial reactive oxygen species (ROS) levels.Rosolutamide has been used in the study of neurodegeneration such as spinal cerebellar ataxia and Huntington disease. neurodegenerative diseases such as Huntington's disease. Regulates oxidative homeostasis.

Ailanthone (AIL) is a natural compound derived from the tree Ailanthus altissima and has anti-hepatocellular carcinoma (HCC) properties. It can induce G0/G1 phase cell cycle arrest by downregulating the expression of cyclins and CDKs, while upregulating the expression of p21 and p27. Additionally, Ailanthone is a potent androgen receptor (AR) inhibitor, capable of inhibiting both the full-length androgen receptor (IC50: 69 nM) and constitutively active splice variants (IC50: 309 nM).

Bifluranol (BX341) has anti-androgenic activity and has shown significant anti-prostatic activity in in vivo studies for the treatment of benign prostatic hyperplasia (BPH).

Apalutamide (ARN-509) is a small molecule androgen receptor (AR) antagonist with potential antineoplastic activity.

Darolutamide (BAY-1841788) is an androgen receptor (AR) antagonist that blocks AR nuclear translocation (Ki: 11 nM).

Ostarine (MK-2866) is a non-steroidal agent with anabolic activity. Selective androgen receptor modulator (SARM) GTx-024 is designed to work like testosterone, thus promoting and/or maintaining libido, fertility, prostate growth, and muscle growth and strength. Mimicking testosterone's action, this agent may increase lean body mass, thereby ameliorating muscle wasting in the hypermetabolic state of cancer cachexia.

MI-136 inhibits expression of androgen receptor (AR) target genes that DHT induced.

ONC1-13B is a potent androgen receptor (AR) antagonist with an ic50 in the range of 59-80 nM that inhibits PSA production in androgen-sensitive human PCa LNCaP cells.

Protodioscin (Furostanol I) is a major steroidal saponin in dioscoreae rhizome, with anti-hyperlipidemia, anti-cancer properties.

ARD-2128 is a highly potent, orally bioavailable PROTAC (proteolysis-targeting chimera) that degrades the androgen receptor (AR), effectively reducing AR protein levels, suppressing AR-regulated gene expression in tumor tissues, and inhibiting tumor growth without evident toxicity. This compound holds promise for prostate cancer research.

Lupeol (Monogynol B) is a novel androgen receptor inhibitor with anti-inflammatory and antioxidant activity.

Procyanidin B3(B3) is a procyanidin dimer that is widely studied due to its high abundance in the human diet and antioxidant activity.

MK-0773 (PF-05314882) is a selective androgen receptor modulator that binds to AR (IC50: 6.6 nM) for the study of diseases caused by endocrine abnormalities.

Triptophenolide (Hypolide) is a compound isolated from Tripterygium wilfordii Hook with anti-inflammatory activity.

N-Desmethyl-Apalutamide is a less potent antagonist of the androgen receptor, is an active Apalutamide metabolite.

VPC-13163 (NSC-52361) has strong anti-proliferative activity against LNCaP and Enzalutamide-resistant prostate cancer cell lines (MR49F) whereas it did not affect the growth of AR independent PC3 cell line. It also inhibits Prostate Specific Antigen (PSA) in both LNCaP and MR49F and reduces expression of AR target genes, PSA and TMPRSS2. These findings suggest that VPC-13566 exhibits AR BF3 specific mechanism of action.

Ralaniten triacetate (EPI-506), a precursor of Ralaniten, is a first-of-its-kind, orally active androgen receptor N-terminal structural domain (AR-NTD) inhibitor with anticancer activity and can be used to study prostate and breast cancer.