1. Signaling Pathways
  2. Cell Cycle/DNA Damage
  3. Checkpoint Kinase (Chk)

Checkpoint Kinase (Chk) (细胞周期检查点激酶)

DNA damage checkpoint and the spindle checkpoint are two cell cycle surveillance systems, which guard against genomic instability. The DNA damage checkpoint kinases CHK1 and CHK2 are central to the induction of cell cycle arrest, DNA repair, and apoptosis as elements in the DNA-damage checkpoint. The components of the spindle checkpoint include Mad1, Mad2, Mad3(BubR1), Bub3 and the kinases Bub1, Mph1(Mps1) and Aurora B.

Cells that suffer DNA damage activate the checkpoint kinases CHK1 and CHK2, which signal to initiate repair processes, limit cell-cycle progression and prevent cell replication, until the damaged DNA is repaired.

The spindle checkpoint causes metaphase arrest when kinetochore-microtubules are unattached during mitosis. The SAC consists of ‘sensor’ proteins, such as Mad1, Bub1 and Mps1; a ‘signal transducer’, consisting of the mitotic checkpoint complex, composed of Mad2, Bub3, BubR1 and Cdc20; and an ‘effector’ known as the anaphase promoting complex/cyclosome (APC/C).

Checkpoint Kinase (Chk) 亚型特异性产品:

  • Chk1

  • Chk2

Checkpoint Kinase (Chk) 相关产品 (8):

目录号 产品名 作用方式 纯度
  • HY-14715B
    CCT241533 hydrochloride Inhibitor 99.98%
    CCT241533 hydrochloride是有效,选择性的 CHK2 抑制剂,IC50Ki 分别为 3 nM 和 1.16 nM。
  • HY-102081
    2OH-BNPP1 Inhibitor 99.65%
    2OH-BNPP1 是一种 BUB1 kinase 抑制剂,可用于癌症研究。
  • HY-117102
    ANI-7 Activator 99.25%
    ANI-7 是一种 AhR 途径的激活剂。ANI-7 抑制多种癌细胞的生长,并有选择地抑制 MCF-7 乳腺癌细胞的生长,GI50 为 0.56 μM。ANI-7 通过激活 AhR 途径诱导 CYP1 代谢单加氧酶,并在敏感的乳腺癌细胞系中诱导 DNA 损伤,检查点激酶 (Chk2) 激活,S 期细胞周期停滞和细胞死亡。
  • HY-107407
    SB-218078 Inhibitor ≥98.0%
    SB-218078 是一种有效的,选择性,ATP 竞争性且细胞可渗透的检查点激酶 1 (Chk1) 抑制剂,可抑制 cdc25C 的 Chk1 磷酸化,IC50 为 15 nM。SB-218078 对 Cdc2 (IC50 为 250 nM) 和 PKC (IC50 为 1000 nM) 的抑制作用较弱。SB-218078 通过 DNA 损伤和细胞周期停滞诱导细胞凋亡。
  • HY-14715
    CCT241533 Inhibitor
    CCT241533 是有效,选择性的 CHK2 抑制剂,IC50Ki 分别为 3 nM 和 1.16 nM。
  • HY-110331
    CCT241533 dihydrochloride Inhibitor
    CCT241533 dihydrochloride 是有效,选择性的 CHK2 抑制剂,IC50Ki 分别为 3 nM 和 1.16 nM。
  • HY-131446
    Chk1-IN-5 Inhibitor
    Chk1-IN-5 是有效的检查点激酶 1 (Chk1) 抑制剂。Chk1-IN-5 抑制 Chk1 磷酸化,并在结肠癌异种移植模型中抑制肿瘤生长。
  • HY-111369
    CHK1-IN-2 Inhibitor
    CHK1-IN-2 是细胞周期检测点激酶 (CHK1) 的抑制剂,其 IC50 为 6 nM。
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