androgenreceptor

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.

Luxdegalutamide (ARV-766) is a novel, potent, and orally bioavailable proteolytic targeting chimera (PROTAC) protein degrader that degrades not only wild-type AR but also clinically relevant AR LBD mutants, including the most prevalent AR L702H, H875Y, and T878A mutations.

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].

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

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 (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.

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

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.

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

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.

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.

Octinoxate (Octyl 4-methoxycinnamate) is used is in sunscreens and other cosmetics to absorb UV-B rays from the sun, protecting the skin from damage,primarily as an ingredient in some sunscreens and lip balms. It is also used to reduce the appearance of scars.

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.

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.

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

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

Cyproterone acetate (Cyproterone 17-O-acetate) binds the androgen receptor (AR), thereby preventing androgen-induced receptor activation in target tissues and inhibiting the growth of testosterone-sensitive tumor cells. Cyproterone acetate is the acetate salt of a synthetic steroidal antiandrogen with weak progestational and antineoplastic activities. This agent also exerts progestational agonist properties at the level of the pituitary that reduce luteinizing hormone (LH), resulting in reductions in testicular androgen secretion and serum testosterone levels. Treatment with cyproterone alone results in incomplete suppression of serum testosterone levels.Cyproterone binds the androgen receptor (AR), thereby preventing androgen-induced receptor activation in target tissues and inhibiting the growth of testosterone-sensitive tumor cells. Cyproterone Acetate is the acetate salt of a synthetic steroidal antiandrogen with weak progestational and antineoplastic activities. This agent also exerts progestational agonist properties at the level of the pituitary that reduce luteinizing hormone (LH), resulting in reductions in testicular androgen secretion and serum testosterone levels. Treatment with cyproterone alone results in incomplete suppression of serum testosterone levels.

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.

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.

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