androgen

Topterone (Win 17,665) is a potent topical antiandrogen that inhibits the stimulation of lumbar organ development by testosterone and dihydrotestosterone in castrated immature male hamsters.

Prochloraz (Prelude) is a broad-spectrum contact imidazole fungicide. Prochloraz inhibits human placental microsomal aromatase in vitro (IC50 = 40 nM). Prochloraz also acts as an estrogen receptor (IC50s = 25 μM) and androgen receptor (IC50 = 4 μM) antagonist, and activates aryl hydrocarbon receptors (EC50 = 1 μM).

RAD140 is an investigational selective androgen receptor modulator (SARM) for the treatment of conditions such as muscle wasting and breast cancer.

D4-abiraterone is the active metabolite of abiraterone produced by 3β-HSD and is further metabolised by SRD5A.Δ4-Abiraterone is an inhibitor of CYP17A1, 3β-HSD and SRD5A, and an antagonist of the androgen receptor.

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.

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

JNJ-63576253 free base (TRC253) is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 can be used for the research of castration-resistant prostate cancer (CRPC).

JNJ-63576253 is a Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC).

Androgen receptor antagonist 1, an orally available full androgen receptor antagonist (IC50: 59 nM), is utilized in the synthesis of PROTAC AR degraders, achieving 24% and 47% AR protein degradation in LNCaP cells at concentrations of 1 μM and 10 μM, respectively.

Androgen receptor degrader-5 (compound 14k) demonstrates superior capabilities, specifically in androgen receptor degradation and antiproliferative activity, showcasing its promising properties.

Androgen receptor antagonist 11 (compound N29) is a selective, orally available antagonist.

Compound EF2 (Androgen receptor antagonist 12) is an orally active antagonist of the androgen receptor (AR) with an IC50 of 0.30 µM. It inhibits the transcriptional activity of mutant AR and the proliferation of AR-positive PCa (prostate cancer) cell lines. Additionally, Compound EF2 blocks the nuclear translocation of AR and suppresses tumor growth in the C4-2B xenograft mouse model. This compound is used for research in prostate cancer.

Androgen receptormodulator 3 is a selective modulator of the androgen receptor, applied in the study of muscle atrophy.

Androgen receptor antagonist 13 (compound 8a) is an orally active androgen receptor antagonist with an IC50 of 0.20 μM. It is used in prostate cancer research.

Androgen receptorligand 1 is a ligand for the androgen receptor (AR). It interacts with the CRBN E3 ligase via a linker to form an AR-PROTAC degrader. This compound is useful in prostate cancer research.

Androgen receptor antagonist 3 (Compound C18) exhibits anticancer activity as an antagonist of the androgen receptor (AR) with an IC50 value of 2.4 μM [1].

Androgen receptor antagonist 4 (Compound AT2) exhibits anticancer activities by potently antagonizing AR transcriptional activity, inhibiting downstream AR target genes, and blocking DHT-induced nuclear translocation of AR. It is an antagonist of the androgen receptor (AR) with an IC50 of 0.15 μM [1].

Androgen receptor antagonist 5 is a potent antagonist of the androgen receptor (AR) (IC50: 6.17 μM). Androgen receptor antagonist 5 inhibited the proliferation of prostate cancer cells LNCaP and showed antitumor effect in LNCaP xenograft mice model, which can be used to study prostate cancer.

Androgen receptor-IN-5 is a potent inhibitor of the androgen receptor with anticancer properties. It additionally suppresses the synthesis of IL-17A, IL-17F, and INF-γ.

Androgen Receptor Degrader-3 (ARD-3) is a compound that inhibits androgen receptor signaling and promotes the degradation of the receptor, with potential applications in prostate cancer research [1].

Androgen Receptor Degrader-1 (Compound 18) is a potent agent for androgen receptor degradation, applicable in cancer research [1].

Androgen Receptor Degrader-2 (Compound 9) is a potent degrader of androgen receptors, with potential application in cancer research [1].

Androgen Receptor Antagonist 9 (compound 28) serves as an antagonist to the androgen receptor [1].

Androgen receptor antagonist 10 (compound 6h) serves as an androgen receptor antagonist that effectively reduces wax esters in the golden Syrian hamster model [1].