map4k

DMX-5804 is a potent, selective MAP4K4 inhibitor, with an IC50 of 3 nM.DMX-5804 enhances cardiomyocyte survival, and reduces ischemia-reperfusion injury in mice.

NG25 is a potent dual inhibitor of TAK1 and MAP4K2, with IC50s of 149 nM and 21.7 nM, respectively.

NCB-0846 is an orally active TNIK inhibitor (IC50: 21 nM).

TAK1 MAP4K2 inhibitor 1 is a potent dual inhibitor of TGFβ-activated kinase 1 (TAK1) and MAP4K2 [IC50s: 41.1 nM and 18.2 nM].

MAP4K4-IN-3 (Compound 17), a serine threonine protein kinase, may be a viable target for antidiabetic agents.

MAP4K4-IN-6 (Compound 15f) is a MAP4K4 inhibitor with an IC50 of 80 nM. It reduces the phosphorylation of c-Jun and exhibits neuroprotective effects. Additionally, MAP4K4-IN-6 enhances the vitality of motor neurons and can be utilized in the study of amyotrophic lateral sclerosis (ALS).

TNIK&MAP4K4-IN-1 (compound A-39) is a potent dual inhibitor of TNIK and MAP4K4 HGK, with IC50 values of 1.29 nM and <10 nM, respectively, in human hepatic stellate cell LX-2, and is applicable in cancer and fibrosis inhibition [1].

GNE-1858 is an ATP-competitive hematopoietic progenitor kinase-1 (HPK1) inhibitor (IC50s of 1.9 nM, 1.9 nM, and 4.5 nM for wild-type and the active mimetic mutants HPK1-TSEE and HPK1-SA).

KY-05009 is a chemical compound that effectively suppresses TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma cells, reduces TNIK protein expression and the transcriptional activity of Wnt target genes, and promotes apoptosis in cancer cells, displaying anti-cancer properties. Furthermore, it functions as an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a Ki of 100 nM.

PF-06260933 is a highly selective small-molecule MAP4K4 inhibitor with IC50s of 3.7 and 160 nM for kinase and cell, respectively.

HPK1-IN-54 (Compound 16) is a potent inhibitor of HPK1 (hematopoietic progenitor kinase 1), enhancing T cell activation and proliferation by blocking HPK1 activity to exert antitumor effects. It has an IC50 of 2.67 nM for HPK1, showing excellent selectivity over the MAP4K family (>100-fold) and other selected kinases (>300-fold). HPK1-IN-54 exhibits moderate in vivo clearance and reasonable oral exposure in both mice and rats. Additionally, in the CT26 mouse colon cancer model, HPK1-IN-54 demonstrates significant antitumor activity and shows a synergistic effect when combined with anti-PD-1 therapy. HPK1-IN-54 holds promise for research in the field of immunology.

Famlasertib is a potent inhibitor of the mitogen-activated protein kinase kinase kinase kinase (MAP4K) family, capable of penetrating the brain. It exhibits an IC50 value of 0.3 nM for HGK (MAP4K4) and 23.7 nM for MLK3.

HPK1-IN-4 is an HPK1 (MAPK41) inhibitor with an IC 50 of 0.061 nM. HPK1-IN-4 is often used as a preclinical immunotherapy tool compound.

HPK1-IN-12 is a potent inhibitor of HPK1. HPK1-IN-12 has potential for the study of HPK1-related diseases.

HPK1-IN-13 is a potent inhibitor of HPK1. HPK1-IN-12 has potential for the study of HPK1-related diseases.

HPK1-IN-14 is a potent inhibitor of HPK1. HPK1-IN-14 has potential for the study of HPK1-related diseases.

HPK1-IN-11 is a potent HPK1 inhibitor. HPK1-IN-11 has potential for the study of HPK1-related diseases.

HPK1-IN-10 is a potent inhibitor of HPK1, a serine threonine protein kinase cloned from hematopoietic progenitor cells and a member of the MAP4K family of mammalian Ste-20-associated protein kinases. HPK1-IN-10 has potential for HPK1-related diseases.

HPK1-IN-9 is a potent HPK1 inhibitor. HPK1 is a serine threonine protein kinase cloned from hematopoietic progenitor cells and is a member of the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-10 has potential for HPK1-related diseases.

HPK1-IN-7 is an orally active HPK1 inhibitor. It shows selectivity against IRAK4 (59 nM) and GLK (140 nM).

GNE-495 is a potent and specific inhibitor of MAP4K4 with an IC50 of 3.7 nM.