Androgen Receptor

<p>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.</p>

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

<p>PROTAC AR-NTD antagonist 1 (compound 18) is a small molecule belonging to the protein-targeting chimeras (PROTACs) that selectively targets the N-terminal</p>

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

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

<p>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.</p>

<p>Ludaterone is an antiandrogen agent, with potent antiandrogenic activity.</p>

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

<p>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.</p>

<p>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.</p>

<p>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.</p>

<p>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.</p>

<p>RLA-4842: iron-based anti-androgen; inhibits mCRPC cell proliferation.</p>

<p>TLB 150 Benzoate (RAD150) is a modulator of the androgen receptor with an IC50 value of 0.13 μM.</p>

<p>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.</p>

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

<p>Lambertianic acid is a bioactive chemical that has anti-allergic and antibacterial effects.</p>

<p>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</p>

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

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

<p>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.</p>

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

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

<p>ACTH, a polypeptide, is secreted by the pituitary gland and regulates cortisol and androgen.</p>

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

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

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

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

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

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

<p>Fenarimol, a pyrimidine-type fungicide, exhibits potent inhibitory activity against BR biosynthesis.</p>

<p>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.</p>

<p>Dehydroepiandrosterone-d2 is a deuterated compound of Dehydroepiandrosterone.</p>

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

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

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

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

<p>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.</p>

<p>VPC-13566 is a BF3-specific small molecule, which effectively inhibited the androgen receptor transcriptional activity and displaced the BAG1L peptide from the</p>

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

<p>AH-3960 是一种甲状腺激素受体 1 (PTHR1) 激动剂。</p>

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

<p>Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist (IC50=36 nM in LNCaP).</p>

<p>Nandrolone phenylpropionate (Nandrolone phenpropionate) is an androgen receptor agonist. It mainly used to treat women with breast cancer and osteoporosis</p>

<p>CTK8A3536 ((2-MORPHOLIN-4-YL-4-PHENYL-1,3-THIAZOL-5-YL)METHANOL) is an inhibitor of Androgen receptor.</p>

<p>MI-136 inhibits expression of androgen receptor (AR) target genes that DHT induced.</p>

<p>Lupeol (Monogynol B) is a novel androgen receptor inhibitor with anti-inflammatory and antioxidant activity.</p>

<p>ARD-2128: potent oral PROTAC that degrades AR, curbing prostate cancer growth with no toxicity.</p>

<p>Dimethylcurcumin (ASC-J9) (ASC-J9) is an androgen receptor degradation enhancer.</p>

<p>Bavdegalutamide (ARV-110) is a PROTAC degrader of androgen receptor (AR).</p>