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MAP4K
MAPK Kinase Kinase Kinase
MAP kinase kinase kinase kinases (MAP4Ks) belong to the mammalian Ste20-like family of serine/threonine kinases. MAP4Ks
including MAP4K1/HPK1, MAP4K2/GCK, MAP4K3/GLK, MAP4K4/HGK, MAP4K5/KHS, and MAP4K6/MINK have been reported to
induce JNK activation through activating the MAP3K-MAP2K cascade. MAP4Ks play important roles in the regulation of cell
apoptosis, cell survival, cell autophagy, and cell migration. Several studies reported that MAP4Ks are involved in the regulation of
immune-cell responses through JNK-independent pathways.
MAP4K1/HPK1 and MAP4K4/HGK play negative roles in T-cell activation and inflammatory responses. In contrast, MAP4K3/GLK
plays a positive role in T-cell activation and autoimmune responses. Moreover, MAP4K1 downregulation and MAP4K3
overexpression in T cells are involved in human autoimmune diseases such as psoriatic arthritis, rheumatoid arthritis (RA),
adult-onset Still’s disease, and SLE.
www.MedChemE 1
MAP4K Inhibitors
DMX-5804 GNE 220
Cat. No.: HY-111754 Cat. No.: HY-U00428
DMX-5804 is a potent, orally active and selective GNE-220 is a potent and selective inhibitor of
MAP4K4 inhibitor, with an IC50 of 3 nM, a pIC50 MAP4K4 with an IC50 of 7 nM.
of 8.55 for human MAP4K4, less potent on
MINK1/MAP4K6 (pIC50, 8.18), and TNIK/MAP4K7
(pIC50, 7.96).
Purity: 99.63% Purity: 98%
Clinical Data: No Development Reported
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