(–)-JJ-450 is a non-competitive antagonist targeting the androgen receptor (AR). It demonstrates superior potency compared to its enantiomer, inhibiting androgen-induced AR activity and exhibiting a distinct mechanism of action that differs from Enzalutamide. (–)-JJ-450 effectively reduces the transcriptional activity of both wild-type AR and the mutant ARF876L by preventing AR nuclear translocation and facilitating the nuclear degradation of unbound AR. This compound is particularly relevant for research into castration-resistant prostate cancer (CRPC) that shows resistance to Enzalutamide.
(–)-JJ-450 is a non-competitive antagonist targeting the androgen receptor (AR). It demonstrates superior potency compared to its enantiomer, inhibiting androgen-induced AR activity and exhibiting a distinct mechanism of action that differs from Enzalutamide. (–)-JJ-450 effectively reduces the transcriptional activity of both wild-type AR and the mutant ARF876L by preventing AR nuclear translocation and facilitating the nuclear degradation of unbound AR. This compound is particularly relevant for research into castration-resistant prostate cancer (CRPC) that shows resistance to Enzalutamide.
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