Androgen Receptor

D4-Abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid 5a-reductase (SRD5A), the main metabolite of abiraterone. D4-Abiraterone is also an antagonist of androgen receptor.

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

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

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.

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

N-Nitrosodicyclohexylamine (NDCHA), an N-nitrosocompound, exhibits anti-androgenic activity by competitively binding to the androgen receptor (AR) in opposition

2-hydroxy Flutamide is competitive inhibition of androgen receptor (AR) for the treatment of prostate cancer

Ralaniten (EPI-002), a potent AR-NTD antagonist, inhibits AR with IC50 of 7.4 μM, for CRPC study.

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

(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

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

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

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

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

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.

Testosterone undecanoate is a metabolite of Testosterone, which is a promising androgen for male hormonal contraception.

LGD-2226: selective oral androgen receptor modulator, EC50: 0.2nM, Ki: 1.5nM. Treats muscle loss, osteoporosis, sexual issues.

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

Topterone (Win 17,665) is a potent topical antiandrogen that inhibits the stimulation of lumbar organ development by testosterone and dihydrotestosterone in

Testosterone acetate (NSC-523836) is a hormone with in vitro antitumor activity.

FL442 is an Androgen Receptor (AR) modulator. This compound exhibits potent inhibitory effects in AR-dependent prostate cancer cells, showing similar suppression efficiency to the traditional antiandrogen drugs Bicalutamide and Enzalutamide. It also maintains antiandrogen activity against the Enzalutamide-resistant AR mutant F876L. The pharmacokinetic properties of FL442 in mice reveal a longer half-life (8 hours), excellent targeting (prostate tissue), and metabolic stability. Additionally, it is effective at inhibiting LNCaP tumor growth at low plasma concentrations (30 ng/mL).

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.

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

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

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

JNJ-63576253 free base (TRC253) is a potent and orally active full antagonist of androgen receptor (AR). JNJ-63576253 can be used for the research of CRPC.

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

MK-3984 is a selective androgen receptor modulator, used in the study of conditions caused by androgen deficiency.

DJ-V-159 is a GPRC6A agonist, targeting the G protein-coupled receptor family C group 6 member A (GPRC6A).

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

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

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

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.

Nandrolone decanoate is an anabolic steroid similar to testosterone, stimulating muscle, bone growth, and red blood cell production.

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

Androgen Receptor Degrader-3 (ARD-3) is a compound that inhibits androgen receptor signaling and promotes the degradation of the receptor, with potential

Celiprolol hydrochloride (Selectrol) is a cardioselective beta-1 adrenergic antagonist that has intrinsic sympathomimetic activity.

Anticancer agent 135 (compound 26h) acts as a potent androgen receptor (AR) antagonist, effectively blocking AR nuclear translocation and inhibiting AR/AR-V7

AS-601811 is a bio-active chemical.

Androgen Receptor Degrader-1 (Compound 18) is a potent agent for androgen receptor degradation, applicable in cancer research [1].

AZD3514 is a potent and oral androgen receptor downregulator with Ki of 2.2 μM and has ability of reducing AR protein expression.Phase 1.

Ralaniten triacetate (EPI-506) is a precursor of Ralaniten, an AR-NTD inhibitor, which can be used in the study of prostate and breast cancer.

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

VPC-14449 is a selective androgen receptor DNA-binding domain (AR-DBD) inhibitor, useful in prostate cancer research.

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 (

CLP-3094 (2-([2-(4-CHLOROPHENOXY)ETHYL]THIO)-1H-BE) is a potent androgen receptor BF3 (binding function 3) inhibitor.

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)

Clascoterone (CB-03-01) is a new topical and peripherally selective androgen antagonist.

RU 59063 is a prototype of a new class of high-affinity nonsteroidal androgen receptor (AR) ligands.

VPC-14228 is a specific AR-DBD inhibitor that acts by inhibiting both Y594A and Q592A mutants.