Androgen Receptor

<p>ACP-105 is a novel and potent nonsteroidal selective androgen receptor modulator (SARM) with partial agonist activity relative to the natural androgen</p>

<p>Cyproterone acetate (Cyproterone 17-O-acetate) binds the androgen receptor (AR), thereby preventing androgen-induced receptor activation in target tissues and</p>

<p>Ligandrol is a novel nonsteroidal, oral SARM that binds to the androgen receptor with high affinity (Ki: 1 nM) and selectivity.</p>

<p>Allylestrenol (Gestanin) is a synthetic steroid with progestational activity.</p>

<p>N-Desmethyl-Apalutamide is a less potent antagonist of the androgen receptor, is an active Apalutamide metabolite.</p>

<p>ORM-15341 is a potent and full antagonist for human AR (hAR)( with IC50 values of 38 nM as shown by transactivation assays in AR-HEK293 cells)</p>

<p>Topilutamide (Fluridil) is a topical nonsteroidal antiandrogen.</p>

<p>Medroxyprogesterone Acetate (Farlutin) is a synthetic progestin that is derived from 17-hydroxyprogesterone. Farlutin is a long-acting contraceptive.</p>

<p>2,2,5,7,8-Pentamethyl-6-Chromanol (PMC) is the anti-oxidant moiety of vitamin E (α-tocopherol), which has potent androgen receptor (AR) signaling modulation and</p>

<p>Nilutamide, a nonsteroidal anti-androgen, treats prostate cancer by blocking androgen receptors, not affecting other hormone receptors.</p>

<p>UT-155 is a selective and potent antagonist of the androgen receptor (AR) (Ki: 267 nM for UT-155 binding to AR-LBD).</p>

<p>Bicalutamide (ICI-176334), a synthetic, nonsteroidal antiandrogen, competitively binds to cytosolic androgen receptors in target tissues, thereby inhibiting the</p>

<p>BMS-986365 (CC-94676) is an orally available, selective and highly potent AR degrader with potential anticancer activity that inhibits AR signaling and suppresses tumor growth for the study of prostate cancer.</p>

<p>Zanoterone is an AR antagonist (androgen receptor).Zanoterone has antitumor activity for the treatment of genitourinary disorders and oncological disorders and</p>

<p>Flutamide (SCH 13521) is an antiandrogen with about the same potency as cyproterone in rodent and canine species.</p>

<p>Adrenocorticotropic hormone TFA is an adrenocorticotropic hormone involved in neurohormonal regulation of the body.</p>

<p>Ostarine (MK-2866) is a non-steroidal SARM mimicking testosterone to boost muscle growth, libido, fertility, and may help prevent muscle wasting in cancer.</p>

<p>AS-601811 is a bio-active chemical.</p>

<p>Andarine (GTx-007) (S-4) is an active partial agonist and an investigational selective androgen receptor modulator (SARM).</p>

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

<p>Spironolactone (SC9420) is an Aldosterone Antagonist. The mechanism of action of spironolactone is as an Aldosterone Antagonist.</p>

<p>Octinoxate (Octyl 4-methoxycinnamate) is an organic compound that is used is in sunscreens and other cosmetics to absorb UV-B rays from the sun.</p>

<p>Luxdegalutamide (ARV-766) is an orally available and effective protein degrader of protein hydrolysis-targeted chimeras (PROTAC).Luxdegalutamide degrades the</p>

<p>UT-34 is a selective and orally active antagonist of second-generation pan-androgen receptor (AR) and degrader(IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild</p>

<p>3,3'-Diindolylmethane (DIM), a small molecule compound, is a proposed Y preventive agent.</p>

<p>AR antagonist 1 is a potent antagonist of the androgen receptor.</p>

<p>SK33 is a potent and tissue selective anti-androgen agent. SK33 reduces androgen receptor (AR) transcriptional activity.</p>

<p>Adrenosterone (11-ketoandrostenedione) is a steroid hormone isolated from the adrenal cortex.</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>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>9,10-Dihydrophenanthrene has inhibitory activity against the androgen receptor and can be used in related research in the field of life sciences.</p>

<p>TD-802, an AR-targeting PROTAC with microsomal stability, shows promise for castration-resistant prostate cancer.</p>

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

<p>MK-0773 FA (MK-0773 FA (606101-58-0 Free base)) is an androgen receptor modulator used for the prevention and treatment of cancer-related muscle wasting.</p>

<p>Linuron herbicide disrupts photosynthesis and acts as an androgen receptor antagonist.</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>Galloylalbiflorin, an AR antagonist with IC50 53.3μM, is sourced from Paeonia lactiflora roots, exhibiting anti-androgenic properties.</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>Inocoterone acetate is a nonsteroidal antiandrogen that binds to the androgen receptor and possesses antiandrogenic activity in animal models.</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>Faznolutamide is an antiandrogen agent [1] [2] .</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>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).</p>

<p>MTX-23, an AR-targeted Proteolysis Targeting Chimera (PROTAC), effectively degrades both AR-V7 and AR-FL, inhibiting the proliferation of CaP cells and inducing</p>

<p>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]</p>

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

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

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

<p>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]</p>

<p>steroidal androgen receptor agonist</p>

<p>BWA-522 is a small molecule, orally available protein-targeting chimera (PROTAC) that potentates the degradation of both full-length androgen receptor (AR-FL)</p>

<p>WCA-814, an androgen receptor (AR) antagonist-Hsp90 inhibitor conjugate, induces degradation of both full-length and AR-V7, exhibiting cytotoxic effects in</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>ARD-2585 is an orally active and selective androgen receptor PROTAC degrader with anticancer activity for the study of prostate cancer.</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>Anticancer agent 135 (compound 26h) acts as a potent androgen receptor (AR) antagonist, effectively blocking AR nuclear translocation and inhibiting AR/AR-V7</p>

<p>(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</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>TLB 150 Benzoate (RAD150) is a modulator of the androgen receptor with an IC50 value of 0.13 μM.</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>RD162 is a non-steroidal antiandrogen (NSAA) specifically binding to the androgen receptor (AR).</p>

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

<p>A unique collection of 531 nuclear receptor signaling targeted compounds for high throughput and high content screening;</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>RLA-4842: iron-based anti-androgen; inhibits mCRPC cell proliferation.</p>

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

<p>2-Ethylhexyl trans-4-methoxycinnamate is a sunscreen agent.</p>

<p>Gridegalutamide exhibits anti-androgen and anti-tumor activities.</p>

<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>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.</p>

<p>PROTAC AR Degrader-4: IAP ligand, linker, AR binder; it's a SNIPER that degrades AR non-genetically.</p>

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

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

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

<p>Fenarimol, a pyrimidine-type fungicide, exhibits potent inhibitory activity against BR biosynthesis.</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>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 (8R912) is a Mouse antibody targeting Androgen receptor. Anti-Androgen receptor Antibody (8R912) can be used in ICC/IF.</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>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>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>Dehydroepiandrosterone-d2 is a deuterated compound of Dehydroepiandrosterone.</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>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>ARD-1676 is an orally administered androgen receptor (AR) PROTAC degrader that combines an AR ligand with a cereblon ligand.</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>Testosterone acetate (NSC-523836) is a hormone with in vitro antitumor activity.</p>

<p>GSK-2881078 is a selective androgen receptor modulato (SARM) that is being evaluated for effects on muscle growth and strength in subjects with muscle wasting.</p>

<p>VPC-13566 inhibits growth in LNCaP, Enzalutamide-resistant MR49F, lowers AR gene, PSA, TMPRSS2 expression, but not in AR-independent PC3 cells.</p>

<p>Lupeol (Monogynol B) is a novel androgen receptor inhibitor with anti-inflammatory and antioxidant activity.</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>DJ-V-159 is a GPRC6A agonist, targeting the G protein-coupled receptor family C group 6 member A (GPRC6A).</p>

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

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

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

<p>RU 58841 (PSK-3841) is a specific androgen receptor antagonist or anti-androgen; RU 58841(PSK-3841) has a significant effect on hair regrowth.</p>

<p>p,p'-DDE (p,p'-dichlorodiphenyldichloroethylene) is a metabolite and degradation product of the organochlorine pesticide DDT</p>

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

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

<p>Apalutamide (ARN-509) is a small molecule and androgen receptor (AR) antagonist with potential antineoplastic activity.</p>

<p>S-23 ((S)-3-(4-chloro-3-fluorophenoxy)-N-(4-cyano-3-(trifluoromethyl)phenyl)-2-hydroxy-2-methylpropanamide) is an oral selective androgen receptor modulator (</p>

<p>Iprodione is a fungicide. Iprodione is also used in cannabis testing kits as a component of pesticide mixes.</p>

<p>Testosterone undecanoate is a metabolite of Testosterone, which is a promising androgen for male hormonal contraception.</p>