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

Mixed Lineage Kinase (混合谱系激酶)

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-149052
    SZM-1209 Inhibitor
    SZM-1209 是一种口服有效且特异性的 RIPK1 抑制剂,Kd 为 85 nM。 SZM-1209 表现出高抗坏死性凋亡(necroptosis) 活性 (EC50=22.4 ± 8.1 nM)。 SZM-1209 具有抗 SIRS (全身炎症反应综合征)和抗 ALI (急性肺损伤)作用。
    SZM-1209
  • HY-156591
    PROTAC MLKL Degrader-1 Degrader
    PROTAC MLKL Degrader-1 (Compound 36) 是一个 MLKLPROTAC 靶向降解剂,Dmax >90%。PROTAC MLKL Degrader-1 包括 修饰的 CRBN 配体、linker和 Lenalidomide (HY-A0003) 接头片段。PROTAC MLKL Degrader-1 能够消除 TSZ 坏死模型中的细胞死亡。
    PROTAC MLKL Degrader-1
  • HY-151541
    MLKL-IN-3 Inhibitor
    MLKL-IN-3 (compound 66) 是一种有效的 MLKL (混合谱系激酶结构域样蛋白)抑制剂。MLKL-IN-3 可抑制 HT-29 细胞的坏死 (necroptosis),作用于 MLKL 磷酸化的下游,其 EC50 为 31 nM。
    MLKL-IN-3
  • HY-149393
    RIPK3-IN-3 Inhibitor
    RIPK3-IN-3 (compound 20) 是 RIP 激酶 (RIP kinase) RIPK3 的选择性抑制剂 (IC50=10 nM)。RIPK3 介导 Mixed Lineage Kinase (MLKL) 磷酸化并引起坏死性凋亡,RIPK3-IN-3 则抑制 p-MLKL 寡聚化从而抑制坏死性凋亡。RIPK3-IN-3 还下调 CXCL5 分泌,抑制 AsPC-1 细胞迁移和侵袭。
    RIPK3-IN-3
  • HY-139878
    MLKL-IN-1 Inhibitor
    MLKL-IN-1 是一种共价 MLKL 抑制剂,KD 值为 50 μM。
    MLKL-IN-1
  • HY-151542
    MLKL-IN-4 Inhibitor
    MLKL-IN-4 (compound 56) 是一种有效的 MLKL (混合谱系激酶结构域样蛋白)抑制剂。MLKL-IN-4 可抑制 HT-29 细胞的坏死 (necroptosis),作用于 MLKL 磷酸化的下游,其 EC50 为 82 nM。
    MLKL-IN-4
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