ARCC 4 is a potent and selective androgen receptor (AR) PROTAC™ Degrader (DC50 = 5 nM). Comprises an androgen receptor antagonist, enzalutamide, joined by a linker to a VHL E3 ligase ligand. Brings about degradation of ARs in VCaP and LNCaP prostate cancer cell lines (Dmax = 98% at 12h) in a proteasome-dependent manner, and inhibits cell proliferation. Also degrades clinically relevant AR mutants expressed in HEK293T cells. Exhibits no significant effect on glucocorticoid, estrogen or progesterone receptors at concentrations inducing AR degradation.
ARCC 4 negative control (Cat. No. 7255) also available.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
