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You are here:Home-Inhibitors & Agonists-Ras-Raf-MAPK-ERK Pathway-MAP4K

Request The Product List ofMAP4K MAP4K

MAP4Ks (Mitogen-activated protein kinase kinase kinase kinases) belong to the mammalian Ste20-like family of serine/threonine kinases. MAP4K family members, including Hematopoietic progenitor kinase 1 (HPK1/MAP4K1), Germinal centre kinase (GCK/MAP4K2), Germinal centre kinase-like kinase (GLK/MAP4K3), HPK/GCK-like kinase (HGK/MAP4K4), Misshapen-like kinase 1 (MINK1/MAP4K6) and TRAF2 and NCK interacting kinase (TNIK/MAP4K7), as potent LATS1/2-activating kinases.

Overexpression or deletion of MAP4Ks affects the phosphorylation and activity of Large tumor suppressor 1/2 (LATS1/2, homologues of Wts) and Yes-associated protein (YAP) /transcriptional co-activator with PDZ-binding motif (TAZ). By acting in a LATS-dependent, but Mammalian Ste20-like kinases 1/2 (MST1/2, homologues of Hpo)-independent manner, MAP4Ks restrict the activity of YAP/TAZ by promoting their phosphorylation and inhibiting target gene expression. MAP4Ks are components of the Hippo pathway by directly phosphorylating and activating the LATS1/2 kinases.MAP4K2/4/6 and MST1/2 both belong to the STE20-like kinase family, and their kinase domains are highly homologous to one another. MAP4K4 acts through LATS to inhibit YAP and cell proliferation.

Cat. No. Product Name CAS No. Information
GY02599

GNE-495

 		1449277-10-4

A potent and highly selective, cell permeable MAP4K4 inhibitor with IC50 of 3.7 nM; exhibits adequate potency preventing migration of HUVEC cells in vitro (IC50=57 nM); has good PK and demonstrates in vivo efficacy in a retinal angiogenesis model .
GY10555

DMX-5804

 		2306178-56-1

DMX-5804 (DMX5804) is a potent, selective small-molecule inhibitor of MAP4K4 with IC50 of 3 nM; displays >100-fold selectivity over GCK/MAP4K2, GLK/MAP4K3, KHS/MAP4K5 and VEGFR; rescues cell survival, mitochondrial function, and calcium cycling in hiPSC-CMs (human induced-pluripotent-stem-cell-derived cardiomyocytes), protects hiPSC-CMs with EC50 of 500 nM for cell death induced by 400 uM H2O2; reduces infarct size and ischemia-reperfusion injury in mice in mice.
GY02376

HG6-64-1

 		1315329-43-1

HG6-64-1 is a potent dual TAK1 and MAP4K2 ((germinal center kinase, GCK)) inhibitor with IC50 of 41 nM and 98 nM, respectively; also inhibits ZAK, p38α, Src, Lyn, CSK and EPH-family kinases (IC50=50-100 nM); inhibits GCK signaling DLBCL cell lines with EC50 of 1.83-157 nM, induces G0/G1 cell-cycle arrest and cell death; inhibits the growth of DLBCL xenograft tumors and prolongs the survival of tumor-bearing mice.
GY02229

GNE-220

 		1199590-75-4

GNE-220 is a potent and selective inhibitor of MAP4K4 with IC50 of 7 nM, also inhibits MINK (MAP4K6), DMPK and KHS1 (MAP4K5) with IC50 of 9 nM, 476 nM and 1,110 nM; alters HUVEC sprout morphology, shifts the distribution of subcellular protrusion and increases total protrusions, dose-dependently increases the number of β1-integrin in long focal adhesions.
GY03846

PF06260933

 		1811510-56-1

PF-06260933 (PF06260933,PF6260933) is a potent, selective, orally available MAP4K4 inhibitor with IC50 of 3.7 nM; demonstrates very good selectivity against more than 150 native kinases, with only the closely related GCK family members (ZC2, TNIK and ZC3, MINK 70% inhibition at 1 uM); inhibits LPS-induced plasma TNFα levels in mouse model.

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