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-182343
    PROTAC MLKL Degrader-3
    		Degrader
    PROTAC MLKL Degrader-3 (compound C116) is a MLKL PROTAC degrader. PROTAC MLKL Degrader-3 induces proteasome- and cereblon-dependent MLKL degradation via ubiquitination. PROTAC MLKL Degrader-3 is applicable to the research of hepatocellular carcinoma.
    PROTAC MLKL Degrader-3
  • HY-181596
    WJH-C19
    		Inhibitor 98.65%
    WJH-C19 is an orally active RIPK1 inhibitor with an IC50 of 5.7 nM. WJH-C19 inhibits the RIPK1/RIPK3/MLKL signaling axis, blocks RIPK1 phosphorylation, suppresses the phosphorylation of downstream RIPK3 and MLKL, disrupts necrosome formation, and exhibits protective effects against necroptosis (Apoptosis) in multiple cell lines. WJH-C19 ameliorates symptoms of inflammatory bowel disease in a mouse colitis model by regulating the necroptosis pathway. WJH-C19 alleviates inflammation and bone destruction in a mouse model of rheumatoid arthritis. WJH-C19 is applicable to research related to inflammatory bowel disease and rheumatoid arthritis.
    WJH-C19
  • 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-139878
    MLKL-IN-1
    		Inhibitor
    MLKL-IN-1 is a covalent MLKL inhibitor with a KD of 50 μM.
    MLKL-IN-1
  • HY-182344
    MLKL ligand-2
    		Ligand
    MLKL ligand-2 is a mixed lineage kinase domain-like pseudokinase (MLKL) PROTAC ligand with a KD of 9.408 μM. MLKL ligand-2 forms hydrogen bond networks and hydrophobic interactions with specific MLKL residues, and stabilizes MLKL in hepatic cells. MLKL ligand-2 can be used to synthesize PROTAC MLKL Degrader-3 (HY-182343).
    MLKL ligand-2
  • HY-180338
    MLK-IN-3
    		Inhibitor
    MLK-IN-3 (Compound 30) is a MLK inhibitor with an IC50 of less than 5 μM. MLK-IN-3 can be used in the research of neurological diseases.
    MLK-IN-3
  • HY-173075
    Anticancer agent 267
    		Activator
    Anticancer agent 267 (Compound 5q) is the activator for RIPK3 and MLKL. Anticancer agent 267 inhibits the proliferation in a variety of cancer cell lines (IC50 for MDA-MB-231, MDA-MB-486 and MCF-7 is 9.79, 10.77 and 5.94 μM, respectively), arrests cell cycle at subG1 phase, and induces necroptosis in cell MDA-MB-231. Anticancer agent 267 exhibits antitumor activity in mouse xenograft models.
    Anticancer agent 267
  • HY-169072
    PROTAC MLKL Degrader-2
    PROTAC MLKL Degrader-2 (compound MP-1) is a PROTAC targeting MLKL (Mixed Lineage Kinase). PROTAC MLKL Degrader-2 is composed of PROTAC target protein ligand PROTAC MLKL Degrader-2 (HY-169072) (red part), E3 ligase ligand Thalidomide (HY-14658) (blue part) and PROTAC Linker N-Methylpiperazine (HY-78871) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is Thalidomide-N-methylpiperazine (HY-169074)[1].
    PROTAC MLKL Degrader-2
  • HY-E70799
    Biotin-MLK1 Recombinant Human Active Protein Kinase
    MLK1 is a kinase for phosphorylation of H3 at threonine 3 and is associated with the osmotic stress response. MLK1 is involved in multiple signaling pathways in the developmental process. Biotin-MLK1 Recombinant Human Active Protein Kinase is obtained by expressing MLK1 proteins and is biotinylated.
    Biotin-MLK1 Recombinant Human Active Protein Kinase
  • 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
  • HY-N0546R
    Ligustroflavone (Standard)
    		Inhibitor
    Ligustroflavone (Standard) is the analytical standard of Ligustroflavone (HY-N0546). This product is intended for research and analytical applications. Ligustroflavone is an orally active flavonoid compound. Ligustroflavone can be extracted from Ligustrum lucidum. Ligustroflavone antagonizes the calcium-sensing receptor (CaSR), inhibits the RIPK1/RIPK3/MLKL pathway, and downregulates TGF-β/Smad signaling. Ligustroflavone regulates calcium metabolism, protects bone tissue, reduces cerebral ischemic injury, and inhibits liver fibrosis. Ligustroflavone can be used in the study of diabetic osteoporosis, ischemic stroke, and liver fibrosis.
    Ligustroflavone (Standard)
  • HY-100573R
    Necrosulfonamide (Standard)
    		Inhibitor
    Necrosulfonamide (Standard) is the analytical standard of Necrosulfonamide (HY-100573). This product is intended for research and analytical applications. Necrosulfonamide is a MLKL and Gasdermin D (GSDMD) inhibitor, capable of separately inhibiting necroptosis and pyroptosis of cells. Necrosulfonamide does not affect the activation of upstream signals, but specifically inhibits the downstream executor oligomerization step. Necrosulfonamide reduces the expression of the key kinases NLRP3 and caspase-1 involved in necroptosis and pyroptosis, activate the Nrf2 pathway and the downstream antioxidant enzymes, and also downregulates a variety of inflammatory factors. Necrosulfonamide plays significant roles in various diseases such as neurodegenerative diseases (such as Parkinson’s disease), tissue damage and ischemia-reperfusion injury, inflammatory bowel disease, osteoarthritis and fracture repair, and hair loss by regulating two important programmed necrosis pathways.
    Necrosulfonamide (Standard)
  • HY-101524R
    TC13172 (Standard)
    		Inhibitor
    TC13172 (Standard) is the analytical standard of TC13172 (HY-101524). This product is intended for research and analytical applications. TC13172 is a mixed lineage kinase domain-like protein (MLKL) inhibitor with an EC50 value of 2 nM for HT-29 cells.
    TC13172 (Standard)
Cat. No. Product Name / Synonyms Application Reactivity