Receptor de andrógenos

Zanoterone is an AR antagonist (androgen receptor).Zanoterone has antitumor activity for the treatment of genitourinary disorders and oncological disorders and

Topilutamide (Fluridil) is a topical nonsteroidal antiandrogen.

SK33 is a potent and tissue selective anti-androgen agent. SK33 reduces androgen receptor (AR) transcriptional activity.

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

3,3'-Diindolylmethane (DIM), a small molecule compound, is a proposed Y preventive agent.

UT-155 is a selective and potent antagonist of the androgen receptor (AR) (Ki: 267 nM for UT-155 binding to AR-LBD).

Cyproterone acetate (Cyproterone 17-O-acetate) binds the androgen receptor (AR), thereby preventing androgen-induced receptor activation in target tissues and

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

Adrenosterone (11-ketoandrostenedione) is a steroid hormone isolated from the adrenal cortex.

BWA-6047 is a dual AR/AR-V7 and GSPT1 PROTAC-type degrader (AR: DC50= 3.7 nM; AR-V7: DC50= 3.0 nM; GSPT1: DC50= 1.2 nM). It facilitates the ubiquitination and degradation of AR/AR-V7 and, through molecular glue properties, induces a PPI between GSPT1 and CRBN, leading to GSPT1 degradation. BWA-6047 is applicable in prostate cancer research.

JJ-450 is a non-competitive antagonist that targets androgen receptors (AR), capable of inhibiting the transcriptional activity of both wild-type AR and mutant ARF876L. It demonstrates an IC50 of approximately 1-10 μM for suppressing AR transcriptional activity in PC3 cells and selectively binds to AR without competing for the ligand binding domain (LBD) with androgens. JJ-450 functions by inhibiting the nuclear translocation of AR and promoting the degradation of unbound ligand AR within the nucleus, thereby suppressing the transcriptional activity of AR and its splice variants, such as ARF876L. This compound can be utilized in studies of castration-resistant prostate cancer (CRPC) that are resistant to Enzalutamide (MDV3100).

Inocoterone acetate is a nonsteroidal antiandrogen that binds to the androgen receptor and possesses antiandrogenic activity in animal models.

ARD-2585 is an orally active and selective androgen receptor PROTAC degrader with anticancer activity for the study of prostate cancer.

Faznolutamide is an antiandrogen agent [1] [2] .

MTX-23, an AR-targeted Proteolysis Targeting Chimera (PROTAC), effectively degrades both AR-V7 and AR-FL, inhibiting the proliferation of CaP cells and inducing

ODM-204 is novel nonsteroidal dual inhibitor of both androgen receptor and CYP17A1 enzyme(IC50s of 80 nM and 22 nM, respectively).

11-Ketodihydrotestosterone is a metabolite of 11β-Hydroxyandrostenedione. It is an active androgen and is also a potent androgen receptor (AR) agonist (Ki: 20.4 nM, EC50: 1.35 nM for human AR).

TD-802, an AR-targeting PROTAC with microsomal stability, shows promise for castration-resistant prostate cancer.

steroidal androgen receptor agonist

LO-4-25 is a covalent degrader targeting the androgen receptor (AR) and its splice variant AR-V7. It covalently binds to the E3 ubiquitin ligase CUL4 DCAF16, facilitating the ubiquitination of both AR and AR-V7, which are then recognized and degraded by the proteasome, leading to reduced protein levels of AR and AR-V7 in cells. LO-4-25 is promising for research on androgen-independent prostate cancer.