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

Checkpoint Kinase (Chk)

Checkpoint Kinase (Chk)

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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) Isoform Specific Products:

Checkpoint Kinase (Chk) Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-19926
    GDC-0425
    		Inhibitor 99.60%
    GDC-0425 (RG-7602) is an orally available, highly selective small molecule ChK1 inhibitor. GDC-0425 can be used for the research of various malignancies.
    GDC-0425
  • HY-125203
    PV-1019
    		Inhibitor 99.30%
    PV-1019 (NSC 744039) is a potent, selective Chk2 inhibitor with an IC50 value of 24 nM. PV-1019 inhibits the Topotecan (HY-13768)-induced Chk2 autophosphorylation. PV-1019 inhibits IR-induced apoptosis.
    PV-1019
  • HY-148962
    LY2880070
    		Inhibitor 98.01%
    LY2880070 is an orally active CHK1 inhibitor, IC50 ＜ 1 nM. LY2880070 can be used as an anticancer agent for combination with DNA damaging agents.
    LY2880070
  • HY-112167A
    GDC-0575 dihydrochloride
    		Inhibitor 99.32%
    GDC-0575 dihydrochloride (ARRY-575 dihydrochloride) is an orally bioavailable CHK1 inhibitor, with an IC50 of 1.2 nM, and has antitumor activity.
    GDC-0575 dihydrochloride
  • HY-100195
    SAR-020106
    		Inhibitor 98.04%
    SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM for human CHK1. SAR-020106 shows excellent selectivity over CHK2. SAR-020106 significantly enhances the cell killing of Gemcitabine and SN38 by 3- to 29-fold in several colon tumor lines and in a p53-dependent fashion. SAR-020106 can enhance antitumor activity with selected anticancer agents.
    SAR-020106
  • HY-15883
    GNE-900
    		Inhibitor 99.21%
    GNE-900 is a an ATP-competitive, selective, and orally active ChK1 inhibitor with IC50s of 0.0011, 1.5 µM for ChKl, ChK2, respectively. GNE-900 abrogates the G2-M checkpoint, enhances DNA damage, and induces Apoptosis.html" class="link-product" target="_blank">Apoptosis. gemcitabine (HY-17026) and GNE-900 administration shows anti-tumor activity.
    GNE-900
  • HY-122198
    ML367
    		Inhibitor 99.84%
    ML367 is a potent inhibitor of ATPase family AAA domain-containing protein 5 (ATAD5) stabilization, acts as a probe molecule that has low micromolar inhibitory activity. ML367 blocks DNA repair pathways, suppresses general DNA damage responses including RPA32-phosphorylation and CHK1-phosphorylation in response to UV irradiation.
    ML367
  • HY-147228
    NR2F6 modulator-1
    		Modulator 99.74%
    NR2F6 modulator-1 is a potent nuclear receptor subfamily 2, group F, member 6 (NR2F6) modulator. NR2F6 modulator-1 can be used for researching immune modulation and modulation of cancer stem cell activity.
    NR2F6 modulator-1
  • HY-117857
    MRT00033659
    		Inhibitor 99.77%
    MRT00033659 is a potent broad-spectrum kinase inhibitor of CK1 (IC50=0.9 μM for CK1δ) and CHK1 (IC50=0.23 μM). MRT00033659, a pyrazolo-pyridine analogue, induces p53 pathway activation and E2F-1 destabilisation.
    MRT00033659
  • HY-117102
    ANI-7
    		Activator 98.13%
    ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells, and potently and selectively inhibits the growth of MCF-7 breast cancer cells with a GI50 of 0.56 μM. ANI-7 induces CYP1-metabolizing mono-oxygenases by activating AhR pathway, and also induces DNA damage, checkpoint Kinase 2 (Chk2) activation, S-phase cell cycle arrest, and cell death in sensitive breast cancer cell lines.
    ANI-7
  • HY-128601
    CHK1-IN-3
    		Inhibitor 99.79%
    CHK1-IN-3 is a Checkpoint Kinase 1 (CHK1) inhibitor with an IC50 of 0.4 nM.
    CHK1-IN-3
  • HY-14715
    CCT241533
    		Inhibitor
    CCT241533 is a potent and selective ATP competitive inhibitor of CHK2 with an IC50 of 3 nM and Ki of 1.16 nM.
    CCT241533
  • HY-18174B
    Prexasertib Mesylate Hydrate
    		Inhibitor
    Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib Mesylate Hydrate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib Mesylate Hydrate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib Mesylate Hydrate shows potent anti-tumor activity.
    Prexasertib Mesylate Hydrate
  • HY-103367
    CHK1-IN-7
    		Inhibitor ≥98.0%
    CHK1-IN-7 (Compound 10c) is a potent human CHK1 inhibitor. CHK1-IN-7 shows no single agent effect, potentiates the antiproliferative effect of Gemcitabine HY-17026 in both prostate and breast cancer cell lines. CHK1-IN-7 can be used for the research of cancer.
    CHK1-IN-7
  • HY-112927
    MU380
    		Inhibitor
    MU380 is a potent and selective CHK1 inhibitor that induces apoptosis and has anticancer activity.
    MU380
  • HY-47026
    Protein kinase inhibitor 6
    		Inhibitor 98.99%
    Protein kinase inhibitor 6 is a protein kinase inhibitor.
    Protein kinase inhibitor 6
  • HY-10992A
    AZD-7762 hydrochloride
    		Inhibitor 99.58%
    AZD-7762 hydrochloride is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC50 of 5 nM for Chk1.
    AZD-7762 hydrochloride
  • HY-139901
    Chk1-IN-6
    		Inhibitor 98.39%
    Chk1-IN-6 is a potent, selective, and orally bioavailable CHK1 inhibitor candidate.
    Chk1-IN-6
  • HY-106009
    VRX0466617
    		Inhibitor 99.91%
    VRX0466617, a selective Chk2 inhibitor, inhibits the phosphorylation of Chk2 Ser 19 and Ser33-35. VRX0466617 can be used in the study of cancer.
    VRX0466617
  • HY-RS02616
    CHEK1 Human Pre-designed siRNA Set A
    		Inhibitor

    CHEK1 Human Pre-designed siRNA Set A contains three designed siRNAs for CHEK1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    CHEK1 Human Pre-designed siRNA Set A
    CHEK1 Human Pre-designed siRNA Set A
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Checkpoint Kinase (Chk) Isoform Comparison

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