map4k4

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.

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].

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

LDC000067 (LDC067) is a highly specific and selective CDK9 inhibitor with an IC50 value of 44±10 nM.

GNE-220 is a potent and selective inhibitor of MAP4K4, with an IC50 of 7 nM.

HPK1-IN-52 is an effective orally active hematopoietic progenitor kinase 1 (HPK1) inhibitor, displaying anti-tumor activity with an IC50 value of 10.4 nM.

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.

PF-06745013 is a potent, MAP4K4-selective inhibitor.

PF-06758955 is a potent, MAP4K4-selective inhibitor.

PF-06260933 Dihydrochloride is a MAP4K4 (HGK) inhibitor (IC50 = 140 nM). It can improve the fasting hyperglycemia in mice. In addition, it inhibited Mink and Tnik (IC50 values of 8 and 13 nM, respectively).

MAP4K4 (HGK) inhibitor (IC50 = 140 nM). Also inhibits MINK and TNIK (IC50 values are 8 and 13 nM, respectively). Improves fasting hyperglycemia in mice. Orally active. Ammirati et al (2015) Discovery of an in vivo tool to establish proof-of-concept for MAP4K4-based antidiabetic treatment. ACS Med.Chem.Lett. 6 1128 PMID:26617966

FLT3 ITD-IN-4 (Compound 16) is a selective inhibitor of FLT3 internal tandem repeat mutations (FLT3-ITD) with an IC50 of 2.3 nM and is applicable for studying acute myeloid leukemia.

GNE 220 (hydrochloride) is a potent and selective MAP4K4 inhibitor with an IC50 of 7 nM.

RET-IN-19 is a potent inhibitor of RET and exhibits anticancer effects on RET-wt (IC50: 6.8 nM) and RET V804M (IC50: 13.51 nM).RET-IN-19 can be used to study non-small cell lung cancer (NSCLC).

F1386-0303 is a novel potent and selective MAP4K4 inhibitor.

ODM-203, a Selective Inhibitor of FGFR and VEGFR, Shows Strong Antitumor Activity, and Induces Antitumor Immunity

ODM-203 sodium is an orally available, selective, and efficient FGFR and VEGFR inhibitor, with antitumor activity, inhibiting FGFR3 1 2 and VEGFR3 2 1 4, inducing antitumor immunity, useful in solid tumor research.

INS018 055 (TNIK&MAP4K4-IN-2) is a highly efficient TNIK and MAP4K4 inhibitor with antifibrotic activity. It can be used in research on idiopathic pulmonary fibrosis.

TGFβRI-IN-3 is a highly selective TGFβR1 inhibitor with an IC50 of 0.79 nM and exhibits 2000-fold selectivity against MAP4K4, showing potential applications in immuno-oncology [1].

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