Receptor de Androgénio

PROTACAR Degrader-10 is a protein degrader targeting androgen receptors (AR) with a DC50 value of ≤100 nM, and can be used in prostate cancer research.

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).

(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

steroidal androgen receptor agonist

17β-hydroxy Exemestane is the primary active metabolite of exemestane .

VAL-201, an androgen receptor antagonist, is used potentially for the treatment of prostate cancer.

ARD-266 is a PROTAC degrader based on the von Hippel-Lindau E3 ligase that induces the degradation of AR proteins and is useful in prostate cancer research.

2-sec-Butylphenol is an inhibitor of the androgen receptor and P450 aromatase, and can be used in research and experiments in the field of life sciences.

A unique collection of xnum nuclear receptor signaling targeted compounds for high throughput and high content screening;

ARD-2051 is a potent, orally active proteolysis-targeting chimera degrader of the androgen receptor (AR), exhibiting DC50 values of 0.6 nM in degrading AR

ATC-324 is a potent autophagy-targeting chimera (AUTOTAC) degrader of the androgen receptor (AR) with a DC50 of 2.05 µM. It induces autophagic-lysosomal degradation of AR, decreases nuclear AR and AR-V7 activity, and exhibits cytotoxic effects on AR-positive prostate cancer cells, making it useful for prostate cancer research.

3-Cl-Pyridine-amide-acrylaldehyde-piperazine serves as a synthetic intermediate for LO-4-25. LO-4-25 is a ligand for the androgen receptor (AR) DNA binding domain and is linked to a truncated fumaramide handle via a connector. In 22Rv1 cells, LO-4-25 demonstrates potent degradation of both AR and AR-V7.

Tibolone is an estrogen-like compound used for the treatment of the symptoms associated with menopausal transition (i.e., climacteric symptoms) and also for the

AR ligand-33 is a ligand for the androgen receptor (AR), and it can be used as a target protein ligand for the synthesis of PROTAC AR Degrader-8.

6-Amino-5-bromoquinoxaline ,with CAS No. 50358-63-9, is a fragment molecule that serves as an important scaffold for molecular linking, expansion, and modification. 6-Amino-5-bromoquinoxaline provides a structural basis and research tool for the design and screening of novel drug candidates, and is commonly used in drug discovery, drug synthesis, and related research.

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.

ACTH, a polypeptide, is secreted by the pituitary gland and regulates cortisol and androgen.

ARD-61: potent PROTAC, degrades AR/PR in AR+ cancers, triggers apoptosis, inhibits tumor growth in mice.

Anticancer agent 135 (compound 26h) acts as a potent androgen receptor (AR) antagonist, effectively blocking AR nuclear translocation and inhibiting AR/AR-V7

WCA-814, an androgen receptor (AR) antagonist-Hsp90 inhibitor conjugate, induces degradation of both full-length and AR-V7, exhibiting cytotoxic effects in