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

Mixed Lineage Kinase (混合谱系激酶)

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.

Mixed Lineage Kinase 相关产品 (6):

目录号 产品名 作用方式 纯度
  • HY-100573
    Necrosulfonamide Inhibitor ≥98.0%
    Necrosulfonamide,一种 necroptosis 抑制剂,通过选择性靶向 (MLKL)。Necrosulfonamide 阻止 MLKL-RIP1-RIP3 坏死小体复合体与其下游效应子相互作用。MLKL 是诱导坏死过程中 RIP3 的重要底物。
  • HY-12599
    URMC-099 Inhibitor 99.90%
    URMC-099 是一种口服生物有效的混合谱系激酶 3 (MLK3) (IC50=14 nM) 抑制剂,具有优异的血脑屏障穿透性。
  • HY-112292
    GW806742X Inhibitor ≥98.0%
    GW806742X 是一种ATP模拟物,是一种有效的 MLKL 抑制剂,结合 MLKL 假激酶结构域,Kd 值为 9.3μM。GW806742X 具有抗 VEGFR2 的活性 (IC50=2 nM)。GW806742X 延缓 MLKL 膜移位并抑制坏死。
  • HY-101524
    TC13172 Inhibitor 99.04%
    TC13172 是 MLKL 的抑制剂,作用于 HT-29 细胞,其 EC50 值为 2 nM。
  • HY-112292A
    GW806742X hydrochloride Inhibitor 98.77%
    GW806742X hydrochloride 是一种ATP模拟物,是一种有效的 MLKL 抑制剂,结合 MLKL 假激酶结构域,Kd 值为 9.3 μM。GW806742X hydrochloride 具有抗 VEGFR2 的活性 (IC50=2 nM)。GW806742X hydrochloride 延缓 MLKL 膜移位并抑制坏死。
  • HY-111351
    MLK-IN-1 Inhibitor
    MLK-IN-1 是一种强效的脑渗透特异性 MLK-3 抑制剂,从专利 US20140256733A1 中获得的化合物 68。
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