Androgen Receptor

RLA-5331: iron activator with anti-androgen properties; inhibits mCRPC cell proliferation.

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]

ARD-69, a potent PROTAC, degrades AR in prostate cancer, with low DC50 values in AR+ cell lines, and suppresses AR gene expression.

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.

Galloylalbiflorin, an AR antagonist with IC50 53.3μM, is sourced from Paeonia lactiflora roots, exhibiting anti-androgenic properties.

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.

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]

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

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.

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.

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.

Ludaterone is an antiandrogen agent, with potent antiandrogenic activity.

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

Dehydroisoandrosterone 3-acetate (Prasterone acetate) is a primary C19 steroid generated by the adrenal cortex.

Dipropyl phthalate is a weak androgen receptor inhibitor, and can be used in biochemical experiments and drug synthesis.

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.

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

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

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

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

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

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

2-Ethylhexyl trans-4-methoxycinnamate is a sunscreen agent.

Gridegalutamide exhibits anti-androgen and anti-tumor activities.

steroidal androgen receptor agonist

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.

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

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

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

Enzalutamide D3 is a deuterium labeled Enzalutamide . Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells.

Anti-Androgen receptor Antibody (8R912) is a Mouse antibody targeting Androgen receptor. Anti-Androgen receptor Antibody (8R912) can be used in ICC/IF.

Anti-Androgen receptor Antibody (7Q574) is an antibody targeting Androgen receptor. Anti-Androgen receptor Antibody (7Q574) can be used in ELISA, WB, IHC.

MK-0773 (PF-05314882) is a selective androgen receptor modulator that binds to AR (IC50: 6.6 nM) for the study of diseases caused by endocrine abnormalities.

Anti-Androgen receptor Antibody (8H883) is an antibody targeting Androgen receptor. Anti-Androgen receptor Antibody (8H883) can be used in ELISA, IHC.

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

Alternariol (Standard) is the standard substance of Alternariol, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Alternariol (AOH), a mycotoxin synthesized by Alternaria species, displays numerous therapeutic and biological effects, including phytotoxic, cytotoxic, anti-HIV, anti-cancer, and anti-microbial properties. It functions by inhibiting the catalytic activity of topoisomerase I and II enzymes.

β-estradiol 17-valerate (EV) is a synthetic estrogen. In hormone replacement therapy drugs, it is widely used in combination with other steroid hormones.

Tricaprin (Standard) is the standard substance of Tricaprin, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Glycerol Tridecanoate is an orally active precursor (DA precursor) of caprylic acid that can be hydrolyzed to caprylic acid. It is a major component of medium chain triglycerides (MCT) and has antiandrogenic and antihyperglycemic properties. It can be used as an additive in food, pharmaceuticals and cosmetics.

Dehydroepiandrosterone-d2 is a deuterated compound of Dehydroepiandrosterone.

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

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

Leelamine hydrochloride, a pine bark extract, inhibits androgen receptor and CB1, reducing lipid synthesis in prostate cancer.

(Rac)-PF-998425: nonsteroidal AR antagonist, potent & selective, IC50: 26 nM (binding), 90 nM (cellular), potential for androgenetic alopecia study.

Apalutamide-13C-d3 is a 13C and 2H labeled Apalutamide. Apalutamide is an androgen receptor (AR) antagonist, used in research on prostate diseases.

Fenarimol, a pyrimidine-type fungicide, exhibits potent inhibitory activity against BR biosynthesis.

Darolutamide (BAY-1841788) is an androgen receptor (AR) antagonist that blocks AR nuclear translocation (Ki: 11 nM).

3-[7 ,7- dimethyl-5-oxo -6H-pyrrolo[3,4-b]pyridin-2-yI]-1H-indole-7 -carbonitrile is an androgen receptor modulator.