(+)-JJ-450

Description

+ -JJ-450 is a non-competitive antagonist targeting the androgen receptor AR that inhibits AR nuclear localization and transcriptional activity in the absence of androgen. + -JJ-450 is less active than - -JJ-450 HY-403733A in inhibiting prostate-specific antigen PSA expression in LN95 cells, possibly because + -JJ-450 targets the ligand binding domain LBD of AR. + -JJ-450 inhibits the transcriptional activity of AR and its splice variants e.g., ARv7 by promoting the degradation of unliganded AR in the nucleus and reducing the binding of AR to androgen response elements AREs . + -JJ-450 can be used in castration-resistant prostate cancer CRPC studies that are resistant to enzalutamide MDV3100 HY-70003 .