1. Signaling Pathways
  2. Cell Cycle/DNA Damage
    Cytoskeleton
  3. MASTL

MASTL (微管相关的丝氨酸/苏氨酸激酶)

Microtubule‐associated serine/threonine kinase like

微管相关丝氨酸/苏氨酸激酶样 (MASTL),也称为 Greatwall (Gwl),是一种重要的有丝分裂激酶,可调节正常或转化细胞的有丝分裂进程。MASTL 激酶最典型的底物是 cAMP 调节的磷蛋白 19 (Arpp19) 和内硫氨酸 α (ENSA,因其与 Arpp19 高度同源而被识别),两者都含有保守的 MASTL 磷酸化基序 FDSGDY。MASTL 的这种激酶功能主要与细胞周期进程有关,它通过下调蛋白磷酸酶 2A (PP2A) 的 B55 亚基来促进有效的有丝分裂退出。这可防止 PP2A 过度去磷酸化和核膜破裂时有丝分裂崩溃。

Microtubule‐associated serine/threonine kinase like (MASTL), also known as Greatwall (Gwl), is an important mitotic kinase that regulates mitotic progression of normal or transformed cells. The best-characterized substrates of MASTL kinase are cAMP-regulated phosphoprotein 19 (Arpp19) and endosulfine alpha (ENSA, identified due to its high homology with Arpp19), both of which contain the conserved MASTL phosphorylation motif FDSGDY. This kinase function of MASTL has primarily been associated with cell-cycle progression, where it facilitates effective mitotic exit through downregulation of the B55 subunit of protein phosphatase 2A (PP2A). This prevents excessive dephosphorylation by PP2A and mitotic collapse upon nuclear envelope breakdown.

MASTL 相关产品 (4):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-137552
    MKI-1 Inhibitor 98.13%
    MKI-1 是微管相关丝氨酸/苏氨酸样激酶 (MASTL) 的抑制剂,其IC50 为9.9 μM。MKI-1 通过激活乳腺癌中的PP2A 发挥抗肿瘤和放射增敏活性。
    MKI-1
  • HY-156715
    MASTL-IN-1 Inhibitor 99.54%
    MASTL-IN-1 是一种 MASTL (微管相关丝氨酸/苏氨酸样激酶) 抑制剂,MASTL 参与细胞的增殖、迁移和侵袭。MASTL-IN-1 具有研究癌症的潜力。
    MASTL-IN-1
  • HY-162732
    MASTL-IN-4 Inhibitor
    MASTL-IN-4 (compound 70) 是一种有效的 MASTL 抑制剂,pIC50 值为 9.15。MASTL-IN-4 表现出抗增殖活性。
    MASTL-IN-4
  • HY-162731
    MASTL-IN-3 Inhibitor
    MASTL-IN-3 (compound 60) 是一种有效的 MASTL 抑制剂,pIC50 值为 9.10 M。MASTL-IN-3 表现出抗增殖活性。
    MASTL-IN-3