Androgen Receptor

EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ～6 μM and a selective PPAR-gamma modulator.

RU 58841 (PSK-3841) is a specific androgen receptor antagonist or anti-androgen; RU 58841(PSK-3841) has a significant effect on hair regrowth.

Spironolactone (SC9420) is an Aldosterone Antagonist. The mechanism of action of spironolactone is as an Aldosterone Antagonist.

Dimethylcurcumin (ASC-J9) (ASC-J9) is an androgen receptor degradation enhancer.

2,2,5,7,8-Pentamethyl-6-Chromanol (PMC) is the anti-oxidant moiety of vitamin E (α-tocopherol), which has potent androgen receptor (AR) signaling modulation and

VPC-13566 is a BF3-specific small molecule, which effectively inhibited the androgen receptor transcriptional activity and displaced the BAG1L peptide from the

Rezvilutamide (SHR3680) is an orally available androgen receptor inhibitor that crosses the blood-brain barrier and has antitumor activity.

ARD-1676 is an orally administered androgen receptor (AR) PROTAC degrader that combines an AR ligand with a cereblon ligand.

AC-262536 is a selective androgen receptor (SAR) modulator and exhibits potent agonist activity at the androgen receptor.

Boldenone Undecylenate (Parenabol) is a synthetic steroid.

D4-Abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid 5a-reductase (SRD5A), the main metabolite of abiraterone. D4-Abiraterone is also an antagonist of androgen receptor.

RD162 is a non-steroidal antiandrogen (NSAA) specifically binding to the androgen receptor (AR).

PROTAC AR-NTD antagonist 1 (compound 18) is a small molecule belonging to the protein-targeting chimeras (PROTACs) that selectively targets the N-terminal

AR antagonist 9 is an orally active, selective androgen receptor (AR) antagonist that inhibits cancer by disrupting the formation of AR ligand-binding domain dimers, showing potential in overcoming drug resistance in prostate cancer (PCa). Its antagonistic activity against AR has an IC50 of 0.051 μM, comparable to Enzalutamide (IC50= 0.060 μM). This compound demonstrates superior inhibitory effects on ARF876L/T877A and ARW741C mutants compared to Enzalutamide. Additionally, AR antagonist 9 possesses favorable pharmacokinetic properties, with an oral bioavailability (F) of 66.24% in rats, and significantly inhibits tumor growth in LNCaP xenograft mouse models upon oral administration. AR antagonist 9 holds promise for research in overcoming PCa resistance.

Ostarine (MK-2866) is a non-steroidal SARM mimicking testosterone to boost muscle growth, libido, fertility, and may help prevent muscle wasting in cancer.

N-Nitrosodicyclohexylamine (NDCHA), an N-nitrosocompound, exhibits anti-androgenic activity by competitively binding to the androgen receptor (AR) in opposition

2-hydroxy Flutamide is competitive inhibition of androgen receptor (AR) for the treatment of prostate cancer

Ralaniten (EPI-002), a potent AR-NTD antagonist, inhibits AR with IC50 of 7.4 μM, for CRPC study.

BWA-522 is a small molecule, orally available protein-targeting chimera (PROTAC) that potentates the degradation of both full-length androgen receptor (AR-FL)

(R)-SKBG-1 is an inhibitor of the RNA-binding protein NONO, effectively downregulating androgen receptor expression by targeting both AR-FL mRNA and AR-V7 mRNA