DMX-5804

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DMX-5804

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

包装与价格：

包装	价格(元)
10mM (in 1mL DMSO)	电议
5mg	电议
10mg	电议

产品介绍

DMX-5804 是一种有效、可口服、选择性的 MAP4K4 抑制剂，对人 MAP4K4 的 IC50 值为 3 nM，pIC50 值为 8.55；对 MINK1/MAP4K6 (pIC50，8.18) 和 TNIK/MAP4K7 (pIC50，7.96) 的作用相对较弱。DMX-5804 能够增强心肌细胞存活率，减少小鼠的缺血再灌注损伤。

MAP4K4

3nM(IC₅₀)

MAP4K4

8.55(pIC₅₀)

MINK1/MAP4K6

8.18(pIC₅₀)

TNIK/MAP4K7

7.96(pIC₅₀)

产品描述

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.