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

Checkpoint Kinase (Chk)

Checkpoint Kinases (Chk) are protein kinases that are involved in cell cycle control. Two checkpoint kinase subtypes have been identified, Chk1 and Chk2. Chk1 is a central component of genome surveillance pathways and is a key regulator of the cell cycle and cell survival. Chk1 is required for the initiation of DNA damage checkpoints and has recently been shown to play a role in the normal (unperturbed) cell cycle. Chk1 impacts various stages of the cell cycle including the S phase, G2/M transition and M phase. In addition to mediating cell cycle checkpoints, Chk1 also contributes to DNA repair processes, gene transcription, embryo development, cellular responses to HIV infection and somatic cell viability. Chk2 is a protein kinase that is activated in response to DNA damage and is involved in cell cycle arrest. In response to DNA damage and replication blocks, cell cycle progression is halted through the control of cell cycle regulators. The protein encoded by this gene is a cell cycle checkpoint regulator and putative tumor suppressor.

Checkpoint Kinase (Chk) Isoform Specific Products:

  • Chk1

  • Chk2

Checkpoint Kinase (Chk) 相关产品 (21):

Cat. No. Product Name Effect Purity
  • HY-18174
    Prexasertib Inhibitor 98.22%
    Prexasertib (LY2606368) 是一种有效,选择性, ATP 竞争性的 Chk1 抑制剂,KiIC50 分别为 <1 nM 和 0.9 nM。
  • HY-10992
    AZD-7762 Inhibitor 99.90%
    AZD-7762 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Chk1的 IC50 为 5 nM。
  • HY-14720
    Rabusertib Inhibitor 99.69%
    Rabusertib (LY2603618) 是一种有效的选择性的 Chk1 抑制剂,IC50 为 7 nM。
  • HY-18958
    CCT245737 Inhibitor 99.24%
    CCT245737 是一种可口服的,选择性的 Chk1 抑制剂,IC50 值为 1.3 nM。
  • HY-18174A
    Prexasertib dihydrochloride Inhibitor 99.41%
    Prexasertib dihydrochloride (LY2606368 dihydrochloride) 是一种有效的,选择性的,ATP 竞争性的 Chk1 抑制剂,Ki 值为 0.9 nM,对 CHK1 和 CHK2 的 IC50 值分别为 <1 nM 和 8 nM。
  • HY-128766
    CHK1-IN-4 Inhibitor
    CHK1-IN-4 (化合物3) 是一种有效的关卡激酶 1 (chk1) 抑制剂,可有效抑制肿瘤细胞中 chk1 磷酸化。CHK1-IN-4 具有抗肿瘤活性。
  • HY-18942
    VER-00158411 Inhibitor
    VER-00158411 是一种 CHK1CHK2 抑制剂,IC50 值分别为 4.4 nM 和 4.5 nM。
  • HY-128601
    CHK1-IN-3 Inhibitor
    CHK1-IN-3 是一种检测点激酶 (CHK1) 抑制剂,IC50 值为 0.4 nM。
  • 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-15532
    SCH900776 Inhibitor 99.97%
    SCH900776 是一种有效,选择性,可口服的 Chk1 抑制剂,IC50 值为 3 nM;它比对CDK2 和 Chk2 的选择性分别高50和500倍。
  • HY-13946
    BML-277 Inhibitor 98.02%
    BML-277 是一种选择性的检测点激酶 2 (Chk2) 抑制剂,IC50 为 15 nM。
  • HY-13263
    CHIR-124 Inhibitor 98.77%
    CHIR-124 是一种有效的,选择性的 Chk1 抑制剂,IC50 值为 0.3 nM;同时可有效抑制 PDGFRFLT3IC50 值分别为 6.6 nM 和 5.8 nM。
  • HY-10032
    PF 477736 Inhibitor 98.07%
    PF 477736 是一种有效的,ATP 竞争性的 Chk1 抑制剂,Ki 为 0.49 nM,对其选择性是 Chk2 (Ki, 47 nM) 的 100 倍。
  • HY-18175
    CCT244747 Inhibitor >99.0%
    CCT244747 是一种有效的,可口服的,高度选择性的 CHK1 抑制剂,IC50 值为 7.7 nM;CCT244747 可废除 G2 检查点,IC50 值为 29 nM。
  • HY-112167
    GDC-0575 Inhibitor >98.0%
    GDC-0575 (ARRY-575, RG7741) 是高选择性,有口服活性的小分子 Chk1 抑制剂,其在异种移植模型中导致肿瘤缩小和生长延迟,IC50 值为1.2 nM。
  • HY-112167A
    GDC-0575 dihydrochloride Inhibitor 99.83%
    GDC-0575 dihydrochloride (ARRY-575 dihydrochloride) 是一种选择性的,可口服的 CHK1 抑制剂,IC50 值为 1.2 nM,具有抗肿瘤活性。
  • HY-14715
    CCT241533 Inhibitor
    CCT241533是高活性丝氨酸/苏氨酸Chk2抑制剂,IC50为3 nM,与其它激酶有极小的交叉反应(1 uM)。
  • HY-104022
    CHK1 inhibitor Inhibitor
    CHK1 inhibitor (GDC-0575 analog) 是 CHK1 的抑制剂。
  • HY-18174B
    Prexasertib Mesylate Hydrate Inhibitor
    Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) 是一种有效、选择性、 ATP 竞争性的 CHK1CHK2 抑制剂,对 CHK1 的 Ki 值为 0.9 nM,IC50 值 <1 nM,对 CHK2 的 IC50 值为 8 nM。Prexasertib Mesylate Hydrate 抑制 HT-29 细胞 CHK1 (S296) 和 CHK2 (S516) 的自身磷酸化。Prexasertib Mesylate Hydrate 具有高效抗肿瘤活性,在 HeLa 细胞中,消除 G2/M 检查点,EC50 值为 9 nM。
  • 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。
Isoform Specific Products

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