ONC1-0013B inhibits AR activity in vitro. A. ONC1-0013B structure. B. LnCAP cells cultured (10% CSS) for 3 days, then treated with tested compounds in presence of 1nM DHT for 1 day. PSA expression plotted as percentage of vehicle control (DMSO; n=2, mean±SEM). Ki values: ± (ONC1-13B), ± (MDV3100), (ARN-509). Mean±SEM from 5 replicate experiments (except ARN-509). C. LnCAP cells cultured (10% CSS) for 3 days, then treated with tested compounds in presence of 1nM DHT for 5 days. Viable cells plotted as percentage of vehicle control (DMSO; n=2, mean±SEM). IC50 values: 30nM (ONC1-13B), 148nM (MDV3100), 240nM (ARN-509). D. Competitive-binding assay vs AR ligand Fluormone™ (PolarScreen™ Androgen Receptor Competitor Assay). IC50 values: 19nM (DHT), (ONC1-13B), (MDV3100).
Anabolic and androgenic steroids are available as prescription medications to be used in cases in which the body does not make enough hormone and supplementation may be required. Some hormone supplements in this pathway include growth hormone and testosterone itself. These medications are legally prescribed by health-care providers, but this group of drugs is often used illegally and abused to help increase athletic performance and improve body appearance. When used in a well-nourished body, anabolic steroids will cause weight gain primarily due to an increase in muscle mass.
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