生物活性 |
DMX-5804 is a potent, orally active and selective MAP4K4 inhibitor, with an IC 50 of 3 nM, a pIC 50 of 8.55 for human MAP4K4, less potent on MINK1/MAP4K6 (pIC 50 , 8.18), and TNIK/MAP4K7 (pIC 50 , 7.96). DMX-5804 enhances cardiomyocyte survival, and reduces ischemia-reperfusion injury in mice.
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体外研究(In Vitro) |
DMX-5804 exhibits great selectivity at MAP4K4 over other kinases, such as GCK/MAP4K2 (pIC50, 6.50), GLK/MAP4K3 (pIC50, 4.95), KHS/MAP4K5 (pIC50, 6.36), ABL1 (pIC50, 5.80), Aurora B (pIC50, 5.49), FLT3 (pIC50, 5.31), GSK3β (pIC50, 4.66), MLK1/MAP3K9 (pIC50, 7.19), MLK3/MAP3K11 (pIC50, 6.99), NUAK (pIC50, 6.88) and VEGFR (pIC50, 5.72). has not independently confirmed the accuracy of these methods. They are for reference only.
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