11-Ketodihydrotestosterone is a metabolite of 11β-Hydroxyandrostenedione. It is an active androgen and is also a potent androgen receptor (AR) agonist (Ki: 20.4 nM, EC50: 1.35 nM for human AR).

Androgen receptor (human):1.35 nM (EC50), Androgen receptor (human):20.4 nM (Ki)

11-Ketodihydrotestosterone (11-KDHT; 1-10 nM; 24 hours; LNCaP and VCaP cells) treatment induces significant cell proliferation. 11-KDHT (0.1-10 nM; 7-10 days; LNCaP and VCaP cells) treatment results in the significant upregulation of KLK3, TMPRSS2 and FKBP5 in both LNCaP and VCaP cells, with the exception of KLK3 at 1 nM in LNCaP cells [1]. In PNT2 cells, only 20% of 11β-hydroxyandrostenedione (11OHA4) and 11β-hydroxytestosterone (11OHT) are metabolized with the former yielding 11keto-androstenedione (11KA4), 11-KDHT and 11β-hydroxy-5α-androstanedione (11OH-5αDIONE) and the latter yielding 11OHA4, 11KT and 11-Ketodihydrotestosterone with downstream products <0.03 μM. In prostate cancer tissue, C11-oxy C19 metabolites at significantly higher levels than the C19 steroids are detected, with unconjugated 11-Ketodihydrotestosterone, 11KT and 11OHA4 levels ranging between 13 and 37.5 ng/g. Analyses of total steroid levels in plasma show significant levels of 11OHA4 (≈230-440 nM), 11KT (≈250-390 nM) and 11-Ketodihydrotestosterone (≈19 nM)[2].

Cell Line: LNCaP and VCaP cells. Concentration: 0.1 nM, 1 nM or 10 nM. Incubation Time: 7 days (LNCaP cells) or 10 days (VCaP cells) [1]