ML281 is a potent and selective STK33 inhibitor with IC50 of 14 nM. ML281 showed a 550-fold selectivity over AurB and greater than 700-fold selectivity over PKA.target: STK33IC50: 14 nM [1]ML281 showed low nanomolar inhibition of purified recombinant STK33 and a distinct selectivity profile as compared to other STK33 inhibitors. Even at the highest concentration tested (10 μM), ML281 had no effect on the viability of KRAS-dependent cancer cells. [2]
ML281 (10 μM; 72 hours) suppresses cell viability of NCI-H446 cells[3].
References:
[1]. We wer M et al. A Potent and Selective Quinoxalinone-Based STK33 Inhibitor Does Not Show Synthetic Lethality in KRAS-Dependent Cells. ACS Med Chem Lett, 2012 Dec 13, 3(12):1034-1038.
[2]. Sun EL, et al. Knockdown of human serine/threonine kinase 33 suppresses human small cell lung carcinoma by blocking RPS6/BAD signaling transduction. Neoplasma. 2017;64(6):869-879.
[3]. Spoonamore J et al. Screen for Inhibitors of STK33 Kinase Activity. National Center for Biotechnology Information (US); 2010-2011 Dec 16.