(+) -JJ-450 is a non-competitive antagonist of the androgen receptor (AR), effectively inhibiting AR nuclear localization and transcriptional activity in the absence of androgen. This compound promotes the degradation of unliganded AR within the nucleus, thereby reducing the binding of AR to androgen response elements (AREs), including its splice variants like ARv7. With lower efficacy than its counterpart, (-)-JJ-450, in suppressing prostate-specific antigen (PSA) expression in LN95 cells, (+)-JJ-450 is particularly relevant for research focused on castration-resistant prostate cancer (CRPC) that exhibits resistance to enzalutamide.
(+) -JJ-450 is a non-competitive antagonist of the androgen receptor (AR), effectively inhibiting AR nuclear localization and transcriptional activity in the absence of androgen. This compound promotes the degradation of unliganded AR within the nucleus, thereby reducing the binding of AR to androgen response elements (AREs), including its splice variants like ARv7. With lower efficacy than its counterpart, (-)-JJ-450, in suppressing prostate-specific antigen (PSA) expression in LN95 cells, (+)-JJ-450 is particularly relevant for research focused on castration-resistant prostate cancer (CRPC) that exhibits resistance to enzalutamide.
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