(+) -JJ-450

(+) -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 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).

1998094-24-8

12352005

Androgen Receptor; Prostaglandin Receptor

GPCR/G Protein; Vitamin D Related/Nuclear Receptor

Cancer

O=C([C@@H]1C[C@@H]1C2=CC=C(C=C2)F)N3CCN(CC3)C4=CC(Cl)=CC=C4C

C21H22ClFN2O

372.86

[1]Cole RN, et al. (+) -JJ-74-138 is a Novel Noncompetitive Androgen Receptor Antagonist. Mol Cancer Ther. 2022 Apr 1;21 (4) :483-492.

Room temperature

http://file.medchemexpress.com/batch_PDF/HY-403733B/

Reference compound1

No Development Reported