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。
货号:ajcx39306
CAS:2306178-56-1
分子式:C21H19N3O3
分子量：361.39
溶解度:DMSO : 125 mg/mL (345.89 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

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)