2. Signaling Pathways
  3. MAPK/ERK Pathway
  4. Mixed Lineage Kinase

Mixed Lineage Kinase

MLKs

Mixed Lineage Kinase

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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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-156591
    PROTAC MLKL Degrader-1
    		Degrader
    PROTAC MLKL Degrader-1 (Compound 36) is a PROTAC degrader of MLKL, with a Dmax ＞90%. PROTAC MLKL Degrader-1 contains modified CRBN ligands, linker and Lenalidomide (HY-A0003)-linker fragments. PROTAC MLKL Degrader-1 abrogates cell death in a TSZ model of necroptosis.
    PROTAC MLKL Degrader-1
  • HY-100573A
    (E/Z)-Necrosulfonamide
    		Inhibitor 98.84%
    (E/Z)-Necrosulfonamide is a racemic compound of Necrosulfonamide (HY-100573). Necrosulfonamide is a necroptosis inhibitor acting by selectively targeting the mixed lineage kinase domain-like protein (MLKL). Necrosulfonamide prevents MLKL-RIP1-RIP3 necrosome complex from interacting with its downstream effectors. MLKL is a critical substrate of RIP3 during the induction of necrosis.
    (E/Z)-Necrosulfonamide
  • HY-149052
    SZM-1209
    		Inhibitor
    SZM-1209 is an orally active, potent and specific RIPK1 inhibitor, with a Kd of 85 nM. SZM-1209 exhibits high anti-necroptotic activity (EC50=22.4 ± 8.1 nM). SZM-1209 shows anti-SIRS (systemic inflammatory response syndrome), and anti-ALI (acute lung injury) effects.
    SZM-1209
  • HY-151541
    MLKL-IN-3
    		Inhibitor
    MLKL-IN-3 (compound 66) is a potent MLKL (Mixed lineage kinase domain-like protein) inhibitor. MLKL-IN-3 inhibits necroptosis in HT-29 cells and acts downstream of MLKL phosphorylation, with EC50 of 31 nM. MLKL-IN-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    MLKL-IN-3
  • HY-148767
    MLKL-IN-5
    		Inhibitor
    MLKL-IN-5 is a potent MLKL inhibitor that mediates necroptosis.
    MLKL-IN-5
  • HY-161361
    MLKL-IN-7
    		Inhibitor
    MLKL-IN-7 (compound 9) is a MLKL inhibitor, and shows anti-necroptosis activity in HT-29 cells with the IC50 of 148.4 nM.
    MLKL-IN-7
  • HY-161271
    MLK-IN-2
    		Inhibitor
    MLK-IN-2 (Compound 9a) is a Mixed Lineage Kinase 3 (MLK3) inhibitor containing 3H-imidazole [4,5-b] pyridine structure. IC50 value is 6 nM. MLK-IN-2 can be used to study cancer and neurodegenerative diseases.
    MLK-IN-2
  • HY-139878
    MLKL-IN-1
    		Inhibitor
    MLKL-IN-1 is a covalent MLKL inhibitor with a KD of 50 μM.
    MLKL-IN-1
  • HY-149393
    RIPK3-IN-3
    		Inhibitor
    RIPK3-IN-3 (compound 20) is a selective inhibitor of RIP kinase RIPK3 (IC50=10 nM). RIPK3 mediates the phosphorylation of Mixed Lineage Kinase (MLKL) and causes necroptosis, while RIPK3-IN-3 inhibits p-MLKL oligomerization and thereby inhibits necroptosis. RIPK3-IN-3 also downregulates CXCL5 secretion and inhibits AsPC-1 cell migration and invasion.
    RIPK3-IN-3
  • HY-151542
    MLKL-IN-4
    		Inhibitor
    MLKL-IN-4 (compound 56) is a potent MLKL (Mixed lineage kinase domain-like protein) inhibitor. MLKL-IN-4 inhibits necroptosis in HT-29 cells and acts downstream of MLKL phosphorylation, with EC50 of 82 nM. MLKL-IN-4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    MLKL-IN-4
Cat. No. Product Name / Synonyms Application Reactivity