YAP PROTAC YZ-6 is a selective Yes-associated protein (YAP) PROTAC degrader with DC50 of 4.3 uM and 8.2 uM in Huh7 and NCI-H226 cells respectively, Dmax value of 97%.
exhibits potent significant reduction in YAP levels-over 80% at 10 μM in NCI-H226 cell line.
YZ-6 inhibits the CTGF expression at a low concentration of 5 μM in NCI-H226 cells.
YZ-6 shows an IC50 of 2.9 uM for growth inhibition on Huh7 cells that overexpress YAP.
YZ-6 is able to induce the degradation of YAP with a DC50 value of 4.3 μM and effectively inhibits CTGF expression dose dependently in the Huh7 cell line.
YZ-6 also degrades TAZ protein like YAP protein in the Huh7 cell line.
YZ-6 can effectively reduce the total expression and concentration of YAP in the cell nucleus.
YZ-6 (35 mg/kg, i.p.) exhibits in vivo antitumor activity in Huh7 cell-derived xenograft, profoundly suppresses YAP expression, markedly reduces the levels of the YAP-TEAD target genes CTGF and CYR61.