Receptor de Androgénio

Lambertianic acid is a bioactive chemical that has anti-allergic and antibacterial effects.

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

PROTAC AR Degrader-9 (Compound c6) is a PROTAC-based degrader specifically targeting the androgen receptor. It effectively degrades the androgen receptor in human dermal papilla cells (HDPC) with a DC50 of 262.38 nM. Additionally, this compound enhances the expression of paracrine factors, such as TGF-β1 and β-catenin, thereby promoting hair regeneration in mouse models. [Pink: ligand for target protein AR ligand-38; Black: linker; Blue: ligand for E3 ligase Cereblon]

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.

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.

K2-B4-5e is a PROTAC compound designed to target the degradation of BRD4 and androgen receptor (AR) through a KLHDC2-based E3 ligase mechanism. It effectively induces rapid and potent degradation of BET family proteins and AR within cells.

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.

ARCC-4: A VHL-recruiting, low-nanomolar (DC50=5nM) AR degrader; outshines enzalutamide; degrades AR mutants resistant to therapy.

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.

RLA-4842: iron-based anti-androgen; inhibits mCRPC cell proliferation.

Linuron herbicide disrupts photosynthesis and acts as an androgen receptor antagonist.

VinclozolinM2-2204 is an androgen receptor AUTOTAC degrader with a DC50 of 200 nM in LNCaP prostate cancer cells. It induces the formation of AR+LC3+ autophagic membranes and is applicable for cancer research.

PROTAC AR Degrader-8 (Compound NP18) functions as a PROTAC degrader targeting the androgen receptor (AR) and effectively degrades AR-FL in both 22Rv1 and LNCaP cells with DC50 values of 0.018 μM and 0.14 μM, respectively. It also degrades AR-V7 in 22Rv1 cells with a DC50 of 0.026 μM. Additionally, PROTAC AR Degrader-8 inhibits the proliferation of 22Rv1 and LNCaP cancer cells, exhibiting IC50 values of 0.038 μM and 1.11 μM. It induces cell cycle arrest at the G2/M phase and triggers apoptosis in 22Rv1 cells (apoptosis). Demonstrating anticancer efficacy, PROTAC AR Degrader-8 shows activity in both mouse and zebrafish models. [Pink: ligand for target protein AR ligand-33; Black: linker; Blue: ligand for E3 ligase Cereblon]

Potent, oral AR-V7 degrader (Compound 6); DC50: 0.32µM; targets AR-DBD via VHL E3; EC50: 0.88µM in 22Rv1 cells.

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.

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

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

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).

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