规格: | 98% |
分子量: | 361.39 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
Background:
DMX-5804 is a potent, orally active and selective MAP4K4 inhibitor, with an IC50 of 3 nM, a pIC50 of 8.55 for human MAP4K4, less potent on MINK1/MAP4K6 (pIC50, 8.18), and TNIK/MAP4K7 (pIC50, 7.96). DMX-5804 enhances cardiomyocyte survival, and reduces ischemia-reperfusion injury in mice[1].
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)[1].
[1]. Fiedler LR, et al. MAP4K4 Inhibition Promotes Survival of Human Stem Cell-Derived Cardiomyocytes and Reduces Infarct Size In Vivo. Cell Stem Cell. 2019 Mar 1. pii: S1934-5909(19)30013-X.
Protocol:
MAP4K4 3nM(IC50) | MAP4K4 8.55(pIC50) | MINK1/MAP4K6 8.18(pIC50) | TNIK/MAP4K7 7.96(pIC50) | GCK/MAP4K2 6.50(pIC50) | KHS/MAP4K5 6.36(pIC50) | GLK/MAP4K3 4.95(pIC50) | MLK1/MAP3K9 7.19(pIC50) | MLK3/MAP3K11 6.99(pIC50) | NUAK 6.88(pIC50) | VEGFR 5.72(pIC50) | ABL1 5.80(pIC50) | AuroraB 5.49(pIC50) | FLT3 5.31(pIC50) | GSK3β 4.66(pIC50) |