2306178-56-1

2306178-56-1 structure

Name: DMX-5804
Chemical Name: DMX-5804
CAS Number: 2306178-56-1
Molecular Formula: C₂₁H₁₉N₃O₃
Molecular Weight: 361.39
Catalog: Signaling Pathways MAPK/ERK Pathway MAP4K
Create Date: 2019-06-01 17:48:26
Modify Date: 2024-01-06 18:00:05
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].

Name	DMX-5804

Description	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].
Related Catalog	Signaling Pathways >> MAPK/ERK Pathway >> MAP4K Research Areas >> Cardiovascular Disease
Target	MAP4K4:3 nM (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) Aurora B:5.49 (pIC50) FLT3:5.31 (pIC50) GSK3β:4.66 (pIC50)
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)[1].
References	[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.