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

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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
H9359

Zabedosertib

 		1931994-81-8

Zabedosertib is a potent serine/ threonine kinase inhibitor.
H7345

PF-06260933

 		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.
H7344

PF 6260933 dihydrochloride

 		1883548-86-4

PF 6260933 is a potent, selective and orally bioavailable MAP4K4 inhibitor with kinase IC50 of 3.7 nM, cell IC50 of 160 nM; possesses excellent kinome selectivity and suitable properties for in vivo pharmacological characterization; significantly improves fasting hyperglycemia (44% reduction in blood glucose, 10 mg/kg, bid); also markedly reduces atherosclerotic lesion area in mice.
H7343

MAP4K4-IN-44

 		1623464-28-7

MAP4K4-IN-44 is a potent, moderately selective small molecule MAP4K4 inhibitor with IC50 of 5 nM in LC3K assay, demonstrates favorable in vivo bioavailability in mouse.
H7342

MAP4K4-IN-37

 		2089334-01-8

MAP4K4-IN-37 is a potent, selective, orally active inhibitor of serine-threonine kinase MAP4K4 with IC50 of 0.4 nM; inhibits the other kinase family members, MINK and TNIK (IC50 of 1.3 and

H7341

MAP4K4-IN-17

 		1811510-58-3

MAP4K4-IN-17 is a potent and highly selective MAP4K4 inhibitor with IC50 of 14.9 nM, showes improved overall drug-like properties compared to PF-06260933; a lead compound for advanced preclinical development.
H7340

MAP4K4-IN-11e

 		1774346-60-9

A potent, selective, ATP-competitive inhibitor of MAP4K4 with IC50 of 1.9 uM, without effect on other stress pathway related kinases; is active at much lower concentration in the cellular neurite outgrowth assay and may exhibit better pharmacokinetic properties.
H7339

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.
H7338

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 .
H7337

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.

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