STIMA-1

STIMA-1 (SH group-targeting compound that induces massive apoptosis) reactivates mutant p53. STIMA-1 can stimulate mutant p53 DNA binding in vitro and induce expression of p53 target proteins and trigger apoptosis in mutant p53-expressing human tumor cells. STIMA-1 is shown to covalently modify free thiols on mutant p53 in H1299-His175 cells and fully restore its DNA binding activity to the level seen with wild-type p53, resulting in upregulation of p53-dependent gene expression, including p21, PUMA, and Bax.