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Mixed Lineage Kinase
MLKs
Mixed lineage kinases (MLKs) are mitogen activated protein kinase kinase kinases (MAPKKKs) with features of both serine-threonine
and tyrosine kinases that regulate the c-Jun N-terminal kinase (JNK) mitogen activated protein kinase (MAPK) signaling cascade,
and also regulate p38 and extracellular signal-regulated kinase (ERK).
MLK3 (MAP3K11) is the most widely expressed MLK family member, and is expressed in neurons (as well as other cell types). At the
cellular level, MLK3 is activated by stress, including reactive oxygen species, ceramide, and TNFα. At the molecular level, it is
activated by Cdc42 and Rac, which interact with MLK3, and can cause it to dimerize via a leucine zipper interface, resulting in
autophosphorylation and enzyme activation.
www.MedChemE 1
Mixed Lineage Kinase Inhibitors Activators
GW806742X GW806742X hydrochloride
Cat. No.: HY-112292 Cat. No.: HY-112292A
GW806742X, an ATP mimetic and a potent MLKL GW806742X hydrochloride, an ATP mimetic and a
(Mixed Lineage Kinase Domain-Like protein) potent MLKL (Mixed Lineage Kinase Domain-Like
inhibitor, binds the MLKL pseudokinase domain with protein) inhibitor, binds the MLKL pseudokinase
a K of 9.3 μM. GW806742X has activity against domain with a K of 9.3 μM. GW806742X
d
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