Triptophenolide is a colorless crystalline plate isolated from ethyl acetate extracts of Tripterygium wilfordii. IC50 value:Target:In vitro: Triptophenolide can remarkably inhibit the delayed type hypersensitivity (DTH) reaction induced by DNCB and BSA; and diminished the peripheral blood ANAE+lymphocytes in rats and micc. Moreover, triptophenolide can dramatically increase the amount of total serum complement and significautly decrcase the serum antibody products (1gG ) of rats and mice. The phagocytosis of perioneal exudate macrophages in mice present double effects in vitro [1].In vivo:
LY2452473 is an orally bioavailable, selective androgen receptor modulator (SARM).
UT-34 is a potent, selective and orally active second-generation pan-androgen receptor (AR) antagonist and degrader with IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively. UT-34 binds to ligand-binding domain (LBD) and function-1 (AF-1) domains and requires ubiquitin proteasome pathway to degrade the AR. UT-34 has anti-prostate cancer efficacy[1][2].
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].
Androgen receptor antagonist 3 (Compound C18) is an androgen receptor (AR) antagonist with an IC50 of 2.4 μM. Androgen receptor antagonist 3 shows anticancer activities[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].
JJH260 is AIG1inhibitor, and inhibit the fluorophosphonate reactivity and fatty acid esters of hydroxy fatty acid (FAHFA) hydrolysis activity of AIG1in HEK293T cells, with IC50 values of 0.50 μM and 0.57 μM, respectively[1].
BX341 is an anti-androgen.
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].
YXG-158 (Compound 23-h) is an orally active AR degrader and CYP17A1 inhibitor. YXG-158 has AR degradation activity with DC50 value of 1.28 μM. YXG-158 can inhibit CYP17A1 with IC50 value of 100 nM. XG-158 can be used for the research of enzalutamide-resistant prostate cancer[1].
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.
CLP-3094 is a potent BF3 (binding function 3)-directed inhibitor of the androgen receptor (AR). CLP-3094 inhibits AR transcriptional activity (IC50=4 μM)[1]. CLP-3094 is a selective, potent GPR142 antagonist[2].
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).
N-Nitrosodicyclohexylamine (NDCHA) is a N-nitrosocompound with anti-androgenic activities. N-Nitrosodicyclohexylamine shows the competitive binding to androgen receptor (AR) against 5α-dihydrotestosterone and decreased the level of AR protein[1].
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.
ACP-105 is an orally available, selective amd potent androgen receptor modulator (SARM), with pEC50s of 9.0 and 9.3 for AR wild type and T877A mutant, respectively.
Androgen receptor degrader-1 (compound 18) is a potent androgen receptor degrader. Androgen receptor degrader-1 can be used in research of cancer[1].
Androst-4-ene-3,17-diol, dipropanoate, (3β,17β)- is the dipropanoate of 4-Androstenediol, a metabolite of testosterone.
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.
A031 is a highly effective PROTAC androgen receptor (AR) degrader with an IC50 value less than 0.25 μM for AR protein degradation. A031 has an inhibitory effect on tumor growth in zebrafish with human prostate cancer (VCaP)[1].
ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice[1].