androgen receptor

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

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

Androgen receptor-IN-5 is a potent inhibitor of the androgen receptor with anticancer properties. It additionally suppresses the synthesis of IL-17A, IL-17F, and INF-γ.

Androgen Receptor Antagonist 9 (compound 28) serves as an antagonist to the androgen receptor [1].

Androgen Receptor Degrader-3 (ARD-3) is a compound that inhibits androgen receptor signaling and promotes the degradation of the receptor, with potential applications in prostate cancer research [1].

Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist (IC50=36 nM in LNCaP) that activates autophagy, exhibits antitumor activity, and is commonly used in treating desmoplasia-resistant prostate cancer.

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

Seviteronel (VT-464) is a novel CYP17 cleavage enzyme inhibitor and androgen receptor antagonist used in breast and prostate cancer research.

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.

ONC1-13B is a potent androgen receptor (AR) antagonist with an ic50 in the range of 59-80 nM that inhibits PSA production in androgen-sensitive human PCa LNCaP cells.

Ralaniten triacetate (EPI-506), a precursor of Ralaniten, is a first-of-its-kind, orally active androgen receptor N-terminal structural domain (AR-NTD) inhibitor with anticancer activity and can be used to study prostate and breast cancer.

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

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

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 (SARM) with a Ki of 1.7 nM. S-23 increases prostate, seminal vesicle, and levator ani muscle weights in castrated rats.

RU 58841 (PSK-3841) is a specific androgen receptor antagonist with significant effects on hair regrowth.

Prochloraz (Prelude) is a broad-spectrum contact imidazole fungicide. Prochloraz inhibits human placental microsomal aromatase in vitro (IC50 = 40 nM). Prochloraz also acts as an estrogen receptor (IC50s = 25 μM) and androgen receptor (IC50 = 4 μM) antagonist, and activates aryl hydrocarbon receptors (EC50 = 1 μM).

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

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

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

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

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

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

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

Ostarine (MK-2866) is a non-steroidal agent with anabolic activity. Selective androgen receptor modulator (SARM) GTx-024 is designed to work like testosterone, thus promoting and/or maintaining libido, fertility, prostate growth, and muscle growth and strength. Mimicking testosterone's action, this agent may increase lean body mass, thereby ameliorating muscle wasting in the hypermetabolic state of cancer cachexia.

Nilutamide (RU23908), an antineoplastic hormonal agent, is mainly used in the treatment of prostate Y. Nilutamide is a pure, nonsteroidal anti-androgen with affinity for androgen receptors, but not for estrogen, progestogen, or glucocorticoid receptors. Therefore, Nilutamide can block the action of androgens of testicular and adrenal origin that stimulate the growth of malignant and normal prostatic tissue. Prostate Y is mainly androgen-dependent and can be treat with chemical castration or surgical. So far, antiandrogen monotherapy has not consistently been certified to be equivalent to castration.

2,2,5,7,8-Pentamethyl-6-Chromanol (PMC) is the antioxidant component of vitamin E (α-tocopherol) and exhibits significant androgen receptor (AR) signaling modulation and anti-cancer activity against prostate cancer cell lines.

Allura Red AC (CI 16035) is a very important food azo dye used in the food, pharmaceutical, paper, cosmetic and textile industries.Allura Red AC promotes susceptibility to experimental colitis via mouse intestinal serotonin.

Atraric acid derivatives as a new chemical lead structure for novel therapeutic compounds as AR antagonists, that can be used for prophylaxis or treatment of prostatic diseases. It inhibits PTP1B activity in a dose-dependent manner with IC50 values of 51.5 uM, suggest that atraric acid has potential to treat diabetes.

Drospirenone (ZK 3059) is a synthetic spironolactone analogue and progestin with progestational and anti-mineralocorticoid activity.

Boldenone Undecylenate (Parenabol) is a synthetic steroid.

Sunset Yellow FCF (Sunset yellow) is an orange azo dye with pH-dependent absorbance.Sunset Yellow FCF is used in food, cosmetics and pharmaceuticals.It is used as a colorant food additive in many food products.They may be cytotoxic and genotoxic, so care must be taken when using these materials as food additives.

AS-601811 is a steroidal 5α-reductase inhibitor and androgen receptor modulator used to study hair loss and acne.

JNJ-63576253 free base (TRC253) is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 can be used for the research of castration-resistant prostate cancer (CRPC).

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

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

MK-0773 FA (MK-0773 FA (606101-58-0 Free base)) is a selective androgen receptor modulator with an IC50 value of 6.6 nM for AR, which can be used for the prevention and treatment of cancer-related muscle wasting.

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

Zanoterone is an AR antagonist (androgen receptor).Zanoterone has antitumor activity for the treatment of genitourinary disorders and oncological disorders and may be used in the study of prostate cancer.

AR antagonist 1 is a potent antagonist of the androgen receptor. It binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266.

CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor), with a Kd of 7.43 µM in SPR assays, directly binding to the OC2-HOX domain. CSRM617 hydrochloride induces apoptosis through the appearance of cleaved Caspase-3 and PARP and is well tolerated in the mouse model of prostate cancer [1].

Ralaniten (EPI-002) is a potent, specific, and orally active antagonist of the androgen receptor N-terminal structural domain (AR-NTD), inhibiting AR transcriptional activity with an IC50 value of 7.4 μM. Ralaniten exhibits anticancer activity and is used to study desmoplasia-resistant prostate cancer (CRPC).

VPC-13566 is a BF3-specific small molecule, which effectively inhibited the androgen receptor transcriptional activity and displaced the BAG1L peptide from the BF3 pocket. VPC-13566 inhibits the growth of various prostate cancer cell lines and reduces the growth of AR-dependent prostate cancer xenograft tumors in mice.

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.

Galeterone (VN 124) is an orally bioavailable small-molecule androgen receptor modulator and CYP17 lyase inhibitor with potential antiandrogen activity. Galeterone exhibits three distinct mechanisms of action: 1) as an androgen receptor antagonist, 2) as a CYP17 lyase inhibitor and 3) by decreasing overall androgen receptor levels in prostate cancer tumors, all of which may result in a decrease in androgen-dependent growth signaling. Localized to the endoplasmic reticulum (ER), the cytochrome P450 enzyme CYP17 (P450C17 or CYP17A1) exhibits both 17alpha-hydroxylase and 17, 20-lyase activities, and plays a key role in the steroidogenic pathway that produces progestins, mineralocorticoids, glucocorticoids, androgens, and estrogens.

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

Medroxyprogesterone Acetate (Farlutin) is a synthetic progestin that is derived from 17-hydroxyprogesterone. It is a long-acting contraceptive that is effective both orally or by intramuscular injection and has also been used to treat breast and endometrial neoplasms.

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-type, F876L and W741L AR, respectively), and has anti-prostate cancer efficacy.

Ailanthone (Δ13-Dehydrochaparrinone) is an effective inhibitor of both full-length androgen receptor (AR) (IC50: 69 nM) and constitutively active truncated AR splice variants (IC50: 309 nM).