Proxalutamide (GT0918) is a potent androgen receptor (AR) antagonist.
Dimethomorph-d8 is the deuterium labeled Dimethomorph[1]. Dimethomorph is a fungicide belongs to the fungicide group of sterol biosynthesis inhibitor. Dimethomorph can inhibit fungal cell wall formation. Dimethomorph also inhibits androgen receptor (AR) activity in MDA-kb2 cells with an IC20 of 0.263 μM[2][3][4].
Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM.
Cyproterone acetate is an androgen receptor (AR) antagonist with IC50 of 7.1 nM, as well as a weak progesterone receptor agonist with weak pro-gestational and glucocorticoid activity. Target: Androgen ReceptorCyproterone acetate clearly shows antagonistic properties, while being a partial agonist also, showing agonism for the AR, with EC50 of 4.0 μM, at relatively high concentrations [1]. In the presence of 10 nM Testosterone, low concentrations of Cyproterone acetate inhibits T-stimulated transcription of 3XHRE-LUC, but at higher concentrations, transcription is stimulated. LH levels in Cyproterone acetate-treated rats do not dip below pretreatment levels, although they does not increase as much in the rats treated with 3.2 mg Cyproterone acetate/kg/day as in those which received 0.2 mg Cyproterone acetate/kg/day [2]. Cyproterone acetate exhibits direct negative effect on reproductive organs weight and significant reducing effect on sperm count and Ca2+ contents. SOD and GST activities significantly decrease in addition to significant increase in NO, MDA contents reflecting the oxidative status of testis in Cyproterone acetate treated rats [3].
VPC-14228 is a potent androgen receptor DNA binding domain (AR-DBD) inhibitor that interferes with the interaction of AR with androgen response elements and effectively blocks AR transcriptional activity. VPC-14228 can be used in prostate cancer research[1].
LY2452473 is an orally bioavailable, selective androgen receptor modulator (SARM).
RD162, a diarylthiohydantoin, is an orally active non-steroidal antiandrogen (NSAA). RD162 specifically binds to androgen receptor (AR). RD162 induces tumor regression in mouse models of castration-resistant human prostate cancer[1].
Rezvilutamide (SHR3680) is an androgen receptor antagonist. Rezvilutamide (SHR3680) is used for the study of prostate cancer[1][2].
Galloylalbiflorin (6′-O-Galloylalbiflorin) is an androgen receptor (AR) antagonist (IC50=53.3 μM) and can be found in the roots of Paeonia lactiflora. Galloylalbiflorin shows anti-androgens activity[1].
Spironolactone is a potent antagonist of the androgen receptor. Target: Androgen ReceptorSpironolactone is a potassium sparing diuretic that acts by antagonism of aldosterone in the distal renal tubules. It is used mainly in the treatment of refractory edema in patients with congestive heart failure, nephrotic syndrome, or hepatic cirrhosis. Its effects on the endocrine system are utilized in the treatments of hirsutism and acne but they can lead to adverse effects. 5% topical spironolactone cream acts as an antiandrogen in human sebaceous glands, competing with DHT receptors and producing a decrease of labelled DHT. At the concentrations used the effect has been only local. No side-effects were recorded during both studies [1]. Patients who received spironolactone had a significant improvement in the symptoms of heart failure, as assessed on the basis of the New York Heart Association functional class (P<0.001). Gynecomastia or breast pain was reported in 10 percent of men who were treated with spironolactone, as compared with 1 percent of men in the placebo group (P<0.001). The incidence of serious hyperkalemia was minimal in both groups of patients [2].
Stanolone benzoate (Androstanolone benzoate) is a synthetic androgen and anabolic steroid[1].
MK-0773 is a selective androgen receptor modulators (SARMs) that binds to AR with an IC50 of 6.6 nM.
ASC-J9 is an androgen receptor degradation enhancer that effectively suppresses castration resistant prostate cancer cell proliferation and invasion.
ODM-201 is a potent androgen receptor (AR) antagonist with an IC50 of 26 nM in AR-HEK293 cells.
Dimethomorph is a morpholine fungicide that inhibits fungal cell wall formation. Dimethomorph inhibits mycelial growth of the oomycete fungi P. citrophthora, P. parasitica, P. capsici, and P. infestans (EC50s=0.14 µg/mL, 0.38 µg/mL, <0.1 µg/mL, and 0.16-0.3 µg/mL, respectively) but is less active against the green algae species C. vulgaris or S. obliquus in vitro (EC50s=47.46 µg/mL and 44.87 µg/mL, respectively). Dimethomorph inhibits androgen receptor (AR) activity in a reporter assay in MDA-kb2 human breast cancer cells but not in a yeast antiandrogen screen (IC20s=0.263 µM and 38.5 µM, respectively).
Androgen receptor degrader-2 (compound 9) is a potent androgen receptor degrader. Androgen receptor degrader-2 can be used in research of cancer[1].
RU 58841 (PSK-3841) is a specific androgen receptor antagonist or anti-androgen. RU 58841 (PSK-3841) has a dramatic effect on hair regrowth.
Androgen receptor degrader-1 (compound 18) is a potent androgen receptor degrader. Androgen receptor degrader-1 can be used in research of cancer[1].
YK11 is a partial agonist of androgen receptor, with osteogenic activity.
CSRM617 hydrochloride (CSRM-617) is a small-molecule inhibitor of the transcription factor ONECUT2 (OC2) with Kd of 7.43 uM in SPR assays, binds to OC2-HOX domain directly; inhibits cell growth and induced apoptosis in vitro in several PC cell lines that expressed moderate to high levels of OC2; significantly downregulates PEG10 protein levels in tumors from mice treated with CSRM617, suppresseses metastasis in 22Rv1 cells implanted subcutaneously nude mice.
(rel)-BMS-641988 is a relative configuration of BMS-641988. BMS-641988 is a potent nonsteroidal androgen receptor antagonist. BMS-641988 has the potential for the research of prostate cancer[1].
Adrenocorticotropic hormone (ACTH) is a polypeptide tropic hormone produced by the anterior pituitary gland. Adrenocorticotropic hormone regulates cortisol and androgen production[1][2].
Andarine (S-4) is an investigational selective androgen receptor modulator (SARM) and an active partial agonist.
Androgen receptor degrader-3 is an androgen receptor degrader. Androgen receptor degrader-3 blocks the process of androgen receptor transduction and also degrades the receptor itself. Androgen receptor degrader-3 can be used for prostate cancer research[1].
PROTAC AR-V7 degrader-2 is an AR-based PROTAC. PROTAC AR-V7 degrader-2 inhibits CaP cellular proliferation by degrading AR-V7 and AR-FL. PROTAC AR-V7 degrader-2 induces apoptosis[1].
Epiandrosterone is a steroid hormone with weak androgenic activity. Epiandrosterone is naturally produced by the enzyme 5α-reductase from the adrenal hormone DHEA.
Acetyl-ACTH (3-24) (human, bovine, rat) is a fragment of proopiomelanocortin (POMC) peptide. POMC peptides such as adrenocorticotrophin (ACTH), which is the precursor of α-MSH, is also an agonist at the MC-1 receptor[1].
ARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer[1].
Cyprodinil-13C6 is the 13C6 labeled Cyprodinil. Cyprodinil is an anilinopyrimidine broad-spectrum fungicide that inhibits the biosynthesis of methionine in phytopathogenic fungi. Cyprodinil inhibits mycelial cell growth of B. cinerea, P. herpotrichoides, and H. oryzae on amino acid-free media (IC50s=0.44, 4.8, and 0.03 µM, respectively). Cyprodinil acts as an androgen receptor (AR) agonist (EC50=1.91 µM) in the absence of the AR agonist DHT and inhibits the androgenic effect of DHT (IC50=15.1 µM).