HTH-01-091 is a potent and selective, cell-permeable, ATP-competitive MELK inhibitor with biochemical IC50 of 10.5 nM.
HTH-01-091 displays no significant activity for PIK3CA, mTOR, GSK3A and CDK7 (IC50>600 nM); exhibits substantially improved kinome selectivity in comparison with OTSSP167.
HTH-01-091 induces MELK degradation, but demonstrates poor antiproliferative effects in basal-like breast cancer cell lines.
