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).

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-161108
    PROTAC Chk1 degrader-1 Degrader
    PROTAC Chk1 degrader-1 (Compound PROTAC-2 ) 是一种有效的 Chk1PROTAC 靶向降解剂,DC50 为 1.33 μM。PROTAC Chk1 degrader-1 可用于癌症的研究。
    PROTAC Chk1 degrader-1
  • 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。
    Chk1-IN-5
  • HY-161383
    CHK1-IN-9 Inhibitor
    CHK1-IN-9 (compound 11) 是一个口服活性的 CHK1 抑制剂,IC50 值为 0.55 nM。CHK1-IN-9 可以增强 DNA 损伤药物对肿瘤细胞的作用,与 Gemcitabine (HY-17026) 具有协同抗癌作用。
    CHK1-IN-9
  • HY-P10367
    Ziptide
    Ziptide 是多种激酶的底物,如 MAPK蛋白激酶 2 (MAPKAPK2, Km = 5 μM)、MAPKAPK3 (Km = 30 μM)、PARK (Km = 40 μM)、checkpoint kinase 1 (Chk1, Km = 5 μM), AMP激活蛋白激酶 (AMPK, Km = 75 μM) 以及钙/钙调素依赖性蛋白激酶 II (CamKII, Km = 300 μM)。
    Ziptide
  • HY-151559
    Zn-DPA-maytansinoid conjugate 1 Inhibitor
    Zn-DPA-maytansinoid conjugate 1 是一种类美坦素偶联物,靶向小分子免疫检查点。Zn-DPA-maytansinoid conjugate 1 可诱导肿瘤生长持续消退,使肿瘤微环境 (TME) 恢复活力、变成“发炎热肿瘤”。
    Zn-DPA-maytansinoid conjugate 1
  • HY-P10574
    Phosphorylated CHKtide
    Phosphorylated CHKtide 是一种源自 CDC25C 的合成肽底物,在 DNA 修复途径之一中被 CHK1/CHK2 磷酸化。Phosphorylated CHKtide 用于细胞周期检查点激酶 1 和 2 (CHK1/CHK2) 以及盐诱导激酶 (SIK) 的测定。
    Phosphorylated CHKtide
  • HY-162367
    FLT3/CHK1-IN-2 Inhibitor
    FLT3/CHK1-IN-2 (Compound 30) 是 FLT3CHK1 的双重抑制剂,对 CHK1、FLT3-WT 和 FLT-D835Y IC50 分别为 25.63、16.39、22.80 nM。FLT3/CHK1-IN-2 具有良好的口服 PK 特性和激酶选择性。FLT3/CHK1-IN-2可用于急性髓系白血病 (AML) 的研究。
    FLT3/CHK1-IN-2
  • 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。
    CCT241533 dihydrochloride
  • HY-156470
    Multi-kinase-IN-6 Inhibitor
    Multi-kinase-IN-6 (compound 10e) 是一种多激酶抑制剂,对 TrkAALK2c-KITEGFRPIM1CK2αCHK1CDK2 显示出良好的酶抑制活性。Multi-kinase-IN-6 显示出针对 MCF7、HCT116 和 EKVX 的抗增殖活性,IC50 值分别为 3.36 μM、1.40 μM 和 3.49 μM。Multi-kinase-IN-6 在 MCF7 和 HCT116 细胞中显示细胞周期阻滞在 G1/S 期和 G1 期,具有良好的凋亡 (apoptosis) 效果。
    Multi-kinase-IN-6
  • HY-158303
    Chk2-IN-2 Inhibitor
    Chk2-IN-2 (compound 2) 是 CHK2 的选择性抑制剂,具有潜在的抗癌活性。
    Chk2-IN-2
  • HY-112477
    Chk2-IN-1 Inhibitor
    Chk2-IN-1 (compound 1) 是一种有效和选择性的 checkpoint kinase 2 (Chk2) 抑制剂,抑制 Chk2Chk1IC50 值分别为 13.5 nM 和 220.4 nM。Chk2-IN-1 可引发强烈的共济失调毛细血管扩张突变 (ATM) 依赖性 Chk2 介导的辐射防护作用。
    Chk2-IN-1
  • HY-164523
    PV1162 Inhibitor
    PV1162 是一种选择性 Chk2 抑制剂,IC50 为 0.29 nM。PV1162 通过靶向 Chk2 中特有的、位于 ATP 结合位点 (腺嘌呤结合区) 后方的门控依赖性疏水口袋来抑制 ATP 与 Chk2 结合,从而抑制了 Chk2 的磷酸化作用。PV1162 在抗癌领域具有潜在应用价值。
    PV1162
  • HY-18174H
    Prexasertib lactate Inhibitor
    Prexasertib lactate 是 Prexasertib (HY-18174) 的乳酸盐形式。Prexasertib lactate 是一种选择性的,ATP 竞争性的第二代细胞周期检测点激酶 1 (CHK1) 抑制剂,Ki 为 0.9 nM,IC50 为 <1 nM。Prexasertib lactate 抑制 CHK2 (IC50=8 nM) 和 RSK1 (IC50=9 nM)。Prexasertib lactate 引起双链 DNA 断裂和复制突变,导致细胞凋亡 (apoptosis)。Prexasertib lactate 具有抗肿瘤活性。
    Prexasertib lactate
  • HY-119699
    PV1115 Inhibitor
    PV1115 is a potent and highly selective Chk2 inhibitor with an IC50 of 0.14 nM, 66000 nM, >100000 nM for Chk2, Chk1 and RSK2, respectively. PV1115 is situated within the ATP-binding pocket of Chk2.
    PV1115
  • HY-103366
    NSC 109555 ditosylate Inhibitor
    NSC 109555 ditosylate 是一种高效的、选择性的、ATP 竞争性检查点激酶 2 (Chk2) 抑制剂,其 IC<sub>50</sub> 为 240 nM。NSC 109555 ditosylate 可用于癌症的研究。
    NSC 109555 ditosylate
  • 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。
    CHK1-IN-2
  • HY-10992A
    AZD-7762 hydrochloride Inhibitor
    AZD-7762 hydrochloride 是一种有效的 ATP 竞争性的细胞周期检测点激酶 (checkpoint kinase,Chk) 抑制剂,抑制 Chk1IC50 为 5 nM。
    AZD-7762 hydrochloride
  • HY-U00345
    CHK-IN-1 Inhibitor
    CHK-IN-1 是一种 CHK1CHK2 的抑制剂,具有抗增殖作用。
    CHK-IN-1
目录号 产品名 / 同用名 种属 表达系统
目录号 产品名 / 同用名 应用 反应物种

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.