ML281

Description: ML-281, a quinoxalinone derivative, is a novel, potent and selective STK33 inhibitor with IC50 value of 14 nM. ML281 was identified from a high-throughput screen using compounds in the Molecular Libraries Small Molecule Repository (MLSMR). It showed low nanomolar inhibition of purified recombinant STK33 and a distinct selectivity profile as compared to other STK33 inhibitors. The KRAS oncogene is found in up to 30% of all human tumors. In 2009, RNAi experiments revealed that lowering mRNA levels of a transcript encoding the serine/threonine kinase STK33 was selectively toxic to KRAS-dependent cancer cell lines, suggesting that small-molecule inhibitors of STK33 might selectively target KRAS-dependent cancers.

References: ACS Med Chem Lett. 2012 Dec 13; 3(12):1034-1038.