產品描述: | 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: STK33 IC50: 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. |
靶點: |
STK33;SerineProtease |
體外研究: |
ML281 (10 μM; 72 hours) suppresses cell viability of NCI-H446 cells. Cell Viability Assay Cell Line: NCI-H446 cells Concentration: 10 μM Incubation Time: 72 hours Result: Suppressed cell viability of NCI-H446 cells. |
參考文獻: |
1. Wewer 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. |
溶解性: |
Soluble in DMSO |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
2.568 ml |
12.838 ml |
25.676 ml |
5 mM |
0.514 ml |
2.568 ml |
5.135 ml |
10 mM |
0.257 ml |
1.284 ml |
2.568 ml |
50 mM |
0.051 ml |
0.257 ml |
0.514 ml |
|
注意: |
部分產品我司僅能提供部分信息,我司不保證所提供信息的權威性,僅供客戶參考交流研究之用。 |