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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.

Products Related to Mixed Lineage Kinase(11)

  • GC15004 structure
    GC15004URMC-099
    CAS: 1229582-33-5
    Purity: >99.50%

    URMC-099, as a 7‐azaindole‐based MLK3 inhibitor with IC 50 of 14 nM, could specifically affect specific Aβ species engaged in disease pathobiology.

  • GC34140 structure
    GC34140TC13172
    CAS: 2093393-05-4
    Purity: >99.00%

    TC13172 is a mixed lineage kinase domain-like protein (MLKL) inhibitor with an EC50 value of 2 nM for HT-29 cells.

  • GC36203 structure
    GC36203GW806742X
    CAS: 579515-63-2
    Purity: >99.50%

    GW806742X, an ATP mimetic and a potent MLKL (Mixed Lineage Kinase Domain-Like protein) inhibitor, binds the MLKL pseudokinase domain with a K D of 9.3μM.

  • GC61454 structure
    GC61454GW806742X hydrochloride
    Purity: >98.50%

    GW806742X hydrochloride, an ATP mimetic and a potent MLKL (Mixed Lineage Kinase Domain-Like protein) inhibitor, binds the MLKL pseudokinase domain with a Kd of 9.3 μM. GW806742X hydrochloride has activity against VEGFR2 (IC50=2 nM). GW806742X hydrochloride retards MLKL membrane translocation and inhibits necroptosis.

  • GC63680 structure
    GC63680MLKL-IN-2
    CAS: 899759-16-1
    Purity: >98%

    MLKL-IN-2 is a MLKL inhibitor extracted from patent WO2021224505A1, compound (i).

  • GC64634 structure
    GC64634MLK-IN-1
    CAS: 1627729-62-7
    Purity: >98%

    MLK-IN-1 is a potent, brain penetrant and specific mixed lineage kinase 3 (MLK-3) inhibitor, compound 68, extracted from patent US20140256733A1.

  • GC69543 structure
    GC69543NecroIr1
    Purity: >98%

    NecroIr1 is an iridium (III) complex that induces necrosis in cisplatin-resistant lung cancer cells (A549R). NecroIr1 selectively accumulates in mitochondria, leading to oxidative stress and loss of mitochondrial membrane potential (MMP). NecroIr1 can activate receptor-interacting protein kinase 3 (RIPK3) and mixed lineage kinase domain-like pseudokinase (MLKL), regulating CDK4 expression.

  • GC69544 structure
    GC69544NecroIr2
    Purity: >98.00%

    NecroIr2 is an iridium (III) complex that induces necrosis in cisplatin-resistant lung cancer cells (A549R). NecroIr2 selectively accumulates in mitochondria, leading to oxidative stress and loss of mitochondrial membrane potential (MMP). NecroIr2 can activate receptor-interacting protein kinase 3 (RIPK3) and mixed lineage kinase domain-like pseudokinase (MLKL), regulating CDK4 expression.

  • GC72756 structure
    GC72756(E/Z)-Necrosulfonamide
    CAS: 432531-71-0
    Purity: >98.00%

    (E/Z)-Necrosulfonamide is a racemic compound of Necrosulfonamide.

  • GC73424 structure
    GC73424PRT062607 acetate
    CAS: 1370261-98-5
    Purity: >99.00%

    PRT062607 (P505-15) acetate is an orally available Syk inhibitor (IC50: 1 nM) that inhibits inflammation and induction Apoptosis.

  • GC78969 structure
    GC78969WJH-C19
    Purity: >98.50%

    WJH-C19 is an orally active RIPK1 inhibitor with an IC 50 of 5.7 nM.