11-Ketodihydrotestosterone

32694-37-4

304.42

10 mM in DMSO

Others

11-Ketodihydrotestosterone (11-KDHT; 5alpha-Dihydro-11-keto testosterone) is an endogenous steroid and a metabolite of 11beta-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a potent androgen receptor (AR) agonist with a K_i of 20.4 nM and an EC₅₀ of 1.35 nM for human AR. 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostate cancer cells^[1][2]. IC50 & Target: Ki: 20.4 nM (Human androgen receptor)^[1]
EC50: 1.35 nM (Human androgen receptor)^[1] In Vitro: 11-Ketodihydrotestosterone (11-KDHT; 1-10 nM; 24 hours; LNCaP and VCaP cells) treatment induces significant cell proliferation^[1].
11-Ketodihydrotestosterone (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 11beta-hydroxyandrostenedione (11OHA4) and 11beta-hydroxytestosterone (11OHT) are metabolised with the former yielding 11keto-androstenedione (11KA4), 11-Ketodihydrotestosterone (11-KDHT) and 11beta-hydroxy-5alpha-androstanedione (11OH-5alphaDIONE) and the latter yielding 11OHA4, 11KT and 11-Ketodihydrotestosterone with downstream products <0.03 uM^[2].
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].