Androgen Receptor

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

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

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

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

Proxalutamide is a potent antagonist of the androgen receptor (AR).

Allylestrenol (Gestanin) is a synthetic steroid with progestational activity.

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)

Chlormadinone acetate (Gestafortin) is an orally active synthetic progestational hormone used often in combinations as an oral contraceptive.

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

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.

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

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

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

Topilutamide (Fluridil) is a topical nonsteroidal antiandrogen.

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

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

Adrenocorticotropic hormone TFA is an adrenocorticotropic hormone involved in neurohormonal regulation of the body.

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

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

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

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

AR antagonist 1 is a potent antagonist of the androgen receptor.

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

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

AS-601811 is a bio-active chemical.

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.

Spironolactone (SC9420) is an Aldosterone Antagonist. The mechanism of action of spironolactone is as an Aldosterone Antagonist.

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

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

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

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

9,10-Dihydrophenanthrene has inhibitory activity against the androgen receptor and can be used in related research in the field of life sciences.

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.

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

Compound PDK0245, with CAS No. 50358-63-9, is a fragment molecule that serves as an important scaffold for molecular linking, expansion, and modification. Compound PDK0245 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.

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).

WCA-814, an androgen receptor (AR) antagonist-Hsp90 inhibitor conjugate, induces degradation of both full-length and AR-V7, exhibiting cytotoxic effects in

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.

Faznolutamide is an antiandrogen agent [1] [2] .

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

17β-hydroxy Exemestane is the primary active metabolite of exemestane .

VAL-201, an androgen receptor antagonist, is used potentially for the treatment of prostate cancer.

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

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

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.

(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

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

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.

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.