| Bioactivity | 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] | ||||||||||||
| Invitro | ML281 (10 μM; 72 hours) suppresses cell viability of NCI-H446 cells[3]. Cell Viability Assay[3] Cell Line: | ||||||||||||
| Name | ML281 | ||||||||||||
| CAS | 1404437-62-2 | ||||||||||||
| Formula | C22H19N3O2S | ||||||||||||
| Molar Mass | 389.47 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |