1. Signaling Pathways
  2. MAPK/ERK Pathway
  3. MAP4K

MAP4K

MAP4Ks (Mitogen-activated protein kinase kinase kinase kinases) belong to the mammalian Ste20-like family of serine/threonine kinases. MAP4K family members, including Hematopoietic progenitor kinase 1 (HPK1/MAP4K1), Germinal centre kinase (GCK/MAP4K2), Germinal centre kinase-like kinase (GLK/MAP4K3), HPK/GCK-like kinase (HGK/MAP4K4), Misshapen-like kinase 1 (MINK1/MAP4K6) and TRAF2 and NCK interacting kinase (TNIK/MAP4K7), as potent LATS1/2-activating kinases.

Overexpression or deletion of MAP4Ks affects the phosphorylation and activity of Large tumor suppressor 1/2 (LATS1/2, homologues of Wts) and Yes-associated protein (YAP) /transcriptional co-activator with PDZ-binding motif (TAZ). By acting in a LATS-dependent, but Mammalian Ste20-like kinases 1/2 (MST1/2, homologues of Hpo)-independent manner, MAP4Ks restrict the activity of YAP/TAZ by promoting their phosphorylation and inhibiting target gene expression. MAP4Ks are components of the Hippo pathway by directly phosphorylating and activating the LATS1/2 kinases.MAP4K2/4/6 and MST1/2 both belong to the STE20-like kinase family, and their kinase domains are highly homologous to one another. MAP4K4 acts through LATS to inhibit YAP and cell proliferation.

MAP4K Isoform Specific Products:

  • MAP4K2/GCK

  • MAP4K3/GLK

  • MAP4K4/HGK

  • MAP4K5/KHS1

  • MAP4K6/MINK1

  • MAP4K7/TNIK

MAP4K 相关产品 (8):

Cat. No. Product Name Effect Purity
  • HY-100830
    NCB-0846 Inhibitor 99.55%
    NCB-0846是具有口服活性的TNIK抑制剂,IC50值为21 nM。
  • HY-100343
    GNE-495 Inhibitor 99.68%
    GNE-495 是有效,选择性的 MAP4K4 抑制剂,IC50 值3.7 nM。
  • HY-111754
    DMX-5804 Inhibitor 99.90%
    DMX-5804 是一种有效、可口服、选择性的 MAP4K4 抑制剂,对人 MAP4K4 的 IC50 值为 3 nM,pIC50 值为 8.55;对 MINK1/MAP4K6 (pIC50,8.18) 和 TNIK/MAP4K7 (pIC50,7.96) 的作用相对较弱。DMX-5804 能够增强心肌细胞存活率,减少小鼠的缺血再灌注损伤。
  • HY-15434
    NG25 Inhibitor 99.35%
    NG25 是一种 TAK1MAP4K2 的双抑制剂,IC50 值分别为 149 nM 和 21.7 nM。
  • HY-19562
    PF-06260933 Inhibitor 98.41%
    PF-06260933 是一种具有口服活性的,高度选择性的 MAP4K4 小分子抑制剂,在激酶实验和细胞实验中的 IC50 值分别为 3.7 和 160 nM。
  • HY-U00428A
    GNE 220 Hydrochloride Inhibitor 98.32%
    GNE 220 (Hydrochloride) 是一种有效的选择性 MAP4K4 抑制剂,其 IC50 值为 7 nM。
  • HY-77251
    TAK1/MAP4K2 inhibitor 1 Inhibitor 99.70%
    TAK1/MAP4K2 inhibitor 1 是一种 TAK1MAP4K2 的双重抑制剂,IC50 值分别为 41.1 nM 和 18.2 nM。
  • HY-124745
    KY-05009 Inhibitor 99.80%
    KY-05009 是一种具有 ATP 竞争性的 TNIK 抑制剂,Ki 为 100 nM。KY-05009 在药理上抑制人肺腺癌细胞中 TGF-β1 诱导的上皮-间质转化。KY-05009 还抑制 TNIK 的蛋白表达和 Wnt 靶基因的转录活性,并诱导癌细胞凋亡。KY-05009 具有抗癌活性。
Isoform Specific Products

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Please try each isoform separately.