Androgen Receptor

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

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

<p>AS-601811 is a bio-active chemical.</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>N-Desmethyl-Apalutamide is a less potent antagonist of the androgen receptor, is an active Apalutamide metabolite.</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>Nilutamide, a nonsteroidal anti-androgen, treats prostate cancer by blocking androgen receptors, not affecting other hormone receptors.</p>

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

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

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

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

<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>Flutamide (SCH 13521) is an antiandrogen with about the same potency as cyproterone in rodent and canine species.</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>Adrenocorticotropic hormone TFA is an adrenocorticotropic hormone involved in neurohormonal regulation of the body.</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>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>RAD140 is an investigational selective androgen receptor modulator (SARM) for the treatment of conditions such as muscle wasting and breast cancer.</p>

<p>Adrenosterone (11-ketoandrostenedione) is a steroid hormone isolated from the adrenal cortex.</p>

<p>Spironolactone (SC9420) is an Aldosterone Antagonist. The mechanism of action of spironolactone is as an Aldosterone Antagonist.</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>3,3'-Diindolylmethane (DIM), a small molecule compound, is a proposed Y preventive agent.</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>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>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>Medroxyprogesterone Acetate (Farlutin) is a synthetic progestin that is derived from 17-hydroxyprogesterone. Farlutin is a long-acting contraceptive.</p>

<p>Bicalutamide (ICI-176334), a synthetic, nonsteroidal antiandrogen, competitively binds to cytosolic androgen receptors in target tissues, thereby inhibiting the</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>A unique collection of 531 nuclear receptor signaling targeted compounds for high throughput and high content screening;</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>ARD-2585 is an orally active and selective androgen receptor PROTAC degrader with anticancer activity for the study of 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>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>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>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>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>Dipropyl phthalate is a weak androgen receptor inhibitor, and can be used in biochemical experiments and drug synthesis.</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>Galloylalbiflorin, an AR antagonist with IC50 53.3μM, is sourced from Paeonia lactiflora roots, exhibiting anti-androgenic properties.</p>

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

<p>Linuron herbicide disrupts photosynthesis and acts as an androgen receptor antagonist.</p>

<p>PROTAC AR Degrader-4: IAP ligand, linker, AR binder; it's a SNIPER that degrades AR non-genetically.</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>ACTH, a polypeptide, is secreted by the pituitary gland and regulates cortisol and androgen.</p>

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

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