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Cat. No. Product Name CAS No. Information
PC-61694

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.

PC-60014

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.

PC-42105

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 .

PC-35005

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 <0.6 nM); possesses a high degree of kinome selectivity against a set of 244 kinases; shows potent cellular potency with IC50 of 222 nM, exhibits substantial suppression of TNFα release on LPS-induced TNFα levels in male C57-BL/6J mice
PC-42954

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.
PC-62937

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.
PC-62936

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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