Catalog No.: PC-21406Not For Human Use, Lab Use Only.
UT-155 is a potent and selective AR degrader (SARD), binds to AR-LBD (Ki=267 nM), degrades and inhibits AR and AR splice variants (AR-SVs), including AR-V7.
UT-155 is a potent and selective AR degrader (SARD), binds to AR-LBD (Ki=267 nM), degrades and inhibits AR and AR splice variants (AR-SVs), including AR-V7. UT-155 potently inhibits the R1881-induced wildtype AR transactivation with 6-10-fold higher potency than enzalutamide. UT-155, but not enzalutamide, inhibits the expression of PSA in LNCaP-EnzR (F876L-AR). UT-155 reduces AR expression and promotes degradation of the AR potentially through proteasome pathway. UT-155 promotes degradation of splice-variants of AR in in 22RV1 cells, inhibits AR-target gene expression. UT-155 binds to AR Activation Function Domain 1 (AF-1) between amino acids 244 and 360 with Kd of 1.32 uM, but not to the LBD. UT-155 inhibits AR- and AR-SV-dependent PCa cell proliferation. UT-155 inhibits growth of AR-SV-dependent prostate cancer xenografts.
