ML-281 is a potent ans selective STK33 inhibitor (IC50 = 14 nM). ML281 showed low nanomolar inhibition of purified recombinant STK33 and a distinct selectivity profile as compared to other STK33 inhibitors. ML281 is a valuable addition to small-molecule probes of STK33. v-Ki-ras2 Kirsten rat sarcoma viral oncogene homolog (KRAS) is the most mutated oncogene, and KRAS mutations have been found in up to 20% of all human tumors. STK33 was selectively toxic to KRAS-dependent cancer cell lines, suggesting that small-molecule inhibitors of STK33 might selectively target KRAS-dependent cancers.
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