生物活性 | |||
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描述 | Death-associated protein kinases (DAPKs) play a central role in programmed cell death such as apoptosis and autophagy and are now emerging as targets for drug discovery in novel therapeutic approaches for ischemic diseases in the brain, heart, kidney, and other organs. TC-DAPK 6 is a potent, selective and ATP-competitive DAPKs inhibitor, acting on DAPK1 and DAPK3 with IC50s of 69 and 225 nM, respectively. In a kinase panel assay, TC-DAPK 6 exhibited much reduced or no activity against a panel of other 48 serine/threonine- or tyrosine-kinases tested to date. TC-DAPK 6 also inhibited P70S6K with an IC50 of 1μM[2]. | ||
作用机制 | TC-DAPK 6 possesses the additional hydrophobic interaction in the ATP binding cavity of DAPK[2]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.62mL 0.72mL 0.36mL |
18.10mL 3.62mL 1.81mL |
36.19mL 7.24mL 3.62mL |
参考文献 |
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