Biological Activity |
PU-WS13 is a selective Grp94 inhibitor, with an EC50 of 0.22 uM. IC50 & Target: EC50: 0.22 uM (Grp94), 7.3 uM (Trap-1), 27.3 uM (Hsp90alpha), 41.8 uM (Hsp90beta)[1] In Vitro: PU-WS13 is a Grp94 inhibitor, with an EC50 of 0.22 uM. PU-WS13 also slightly suppresses Hsp90alpha, Hsp90beta and Trap-1, with EC50s of 27.3, 41.8 and 7.3 uM, respectively. PU-WS13 (2.5-20 uM) shows no toxicity on two nonmalignant cell lines. PU-WS13 (15 uM) disrupts the circular architecture of HER2 at the plasma membrane of SKBr3 cells mediated through Grp94. PU-WS13 inhibits Grp94, and the inhibition induces apoptosis in and reduce the viability of HER2 overexpressing breast cancer cells[1]. |