Androgen Receptor

AR antagonist 10 (Compound Y5) is a potent, orally active androgen receptor (AR) antagonist with an IC50 value of 0.04 μM. It demonstrates a dual mechanism of action: antagonizing AR by disrupting AR dimerization and inducing AR degradation through the ubiquitin-proteasome pathway. This compound shows excellent activity against various resistant AR mutants and effectively inhibits the growth of LNCaP xenograft tumors. AR antagonist 10 is applicable for research in resistant prostate cancer.

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

ONC1-13B, an androgen receptor antagonist, is used potentially for the treatment of prostate cancer.

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

LY2452473 (OPK 88004) is an orally available and selective androgen receptor modulator with potential anticancer activity for the study of prostate cancer.

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

Compound EF2 (Androgen receptor antagonist 12) is an orally active antagonist of the androgen receptor (AR) with an IC50 of 0.30 µM. It inhibits the transcriptional activity of mutant AR and the proliferation of AR-positive PCa (prostate cancer) cell lines. Additionally, Compound EF2 blocks the nuclear translocation of AR and suppresses tumor growth in the C4-2B xenograft mouse model. This compound is used for research in prostate cancer.

LX1, an anti-prostate cancer compound, specifically targets the androgen receptor (AR), AR variants, and the steroidogenic enzyme AKR1C3. It inhibits AKR1C3's enzymatic function, decreases the conversion of androstenedione to testosterone, and reduces the expression of both AR and AR-V7, subsequently downregulating their target genes. Additionally, LX1 is effective in overcoming tumor cell resistance to Enzalutamide, and when combined with Enzalutamide, it further suppresses tumor growth.

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

Pentomone (LY-113935) is an anti-androgen compound that acts as a prostate growth inhibitor.

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

Bavdegalutamide (ARV-110) is a PROTAC degrader of androgen receptor (AR).

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

Bifluranol (BX341) has anti-androgenic activity and has shown significant anti-prostatic activity in in vivo studies for the treatment of benign prostatic

Gridegalutamide exhibits anti-androgen and anti-tumor activities.

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

(+)-JJ-74-138 is a novel non-competitive androgen receptor (AR) antagonist capable of inhibiting enzalutamide-resistant castration-resistant prostate cancer (CRPC).

YXG-158 (Compound 23-h), an orally active androgen receptor (AR) degrader and cytochrome P450 17A1 (CYP17A1) inhibitor, exhibits AR degradation with a DC50 of 1

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

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

BMS-641988 is a novel nonsteroidal androgen receptor antagonist for the treatment of prostate cancer.

N-desmethyl Enzalutamide (N-desmethyl MDV 3100) is the active Enzalutamide metabolite.It is the active metabolite of Enzalutamide.

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

Triptophenolide (Hypolide) is a compound isolated from Tripterygium wilfordii Hook with anti-inflammatory activity.

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

GLPG0492 is a novel selective androgen receptor modulator.

Androgen receptor degrader-5 (compound 14k) demonstrates superior capabilities, specifically in androgen receptor degradation and antiproliferative activity, showcasing its promising properties.

GDC-2992 is a selective and oral AR (androgen receptor) degrader that, degrades AR and inhibits proliferation in VCaP cells, prostate cancer (CRPC).

Androgen Receptor Degrader-2 (Compound 9) is a potent degrader of androgen receptors, with potential application in cancer research [1].

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

Ailanthone (Δ13-Dehydrochaparrinone) is an effective inhibitor of both full-length androgen receptor (AR) (IC50: 69 nM) and constitutively active truncated AR

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.

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

Isoquinoline, 5-iodo- (9CI) is a potent and selective inhibitor of SARM1(IC50 = 75 nM) by preventing axonal degeneration and by allowing functional recovery of

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

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

Masofaniten (EPI-7386) is an orally active androgen receptor (AR) inhibitor with antitumor activity for the study of prostate and breast cancer.

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

Enzalutamide carboxylic acid is an antagonist of androgen receptor (AR) .

Androgen receptor-IN-5 is a potent inhibitor of the androgen receptor with anticancer properties.

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

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

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

Dimethylcurcumin (ASC-J9) (ASC-J9) is an androgen receptor degradation enhancer.

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

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

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

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

AC-262536 is a selective androgen receptor (SAR) modulator and exhibits potent agonist activity at the androgen receptor.

Boldenone Undecylenate (Parenabol) is a synthetic steroid.

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.