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-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-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-18174C
    Prexasertib mesylate
    		Inhibitor
    Prexasertib mesylate (LY2606368 mesylate) 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 inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib mesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib mesylate shows potent anti-tumor activity.
    Prexasertib mesylate
  • HY-128766
    CHK1-IN-4
    		Inhibitor
    CHK1-IN-4 (Compound 3) is a potent checkpoint kinase 1 (chk1) inhibitor, and potently inhibits chk1 phosphorylation in the tumor cells. CHK1-IN-4 has anti-tumor activity.
    CHK1-IN-4
  • HY-111369
    CHK1-IN-2
    		Inhibitor
    CHK1-IN-2 is a checkpoint kinase 1 (CHK1) inhibitor, with an IC50 of 6 nM.
    CHK1-IN-2
  • HY-131446
    Chk1-IN-5
    		Inhibitor
    Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model.
    Chk1-IN-5
  • HY-P4978
    CBP501 Affinity Peptide
    		Inhibitor
    CBP501 Affinity Peptide is a Chk kinase inhibitor that can abrogate G2 arrest induced by DNA-damaging agents. CBP501 Affinity Peptide can be used in cancer research.
    CBP501 Affinity Peptide
  • HY-151559
    Zn-DPA-maytansinoid conjugate 1
    		Inhibitor
    Zn-DPA-maytansinoid conjugate 1 is a small molecule-based maytansinoid conjugate targeting immune checkpoint. Zn-DPA-maytansinoid conjugate 1 induces lasting regression of tumor growth and rejuvenates tumor microenvironment (TME) to an “inflamed hot tumor”.
    Zn-DPA-maytansinoid conjugate 1
  • HY-112477
    Chk2-IN-1
    		Inhibitor
    Chk2-IN-1 (compound 1) is a potent and selective inhibitor of checkpoint kinase 2 (Chk2), with IC50s of 13.5 nM and 220.4 nM for Chk2 and Chk1, respectively. Chk2-IN-1 can elicit a strong ataxia telangiectasia mutated (ATM)-dependent Chk2-mediated radioprotection effect.
    Chk2-IN-1
  • HY-112167B
    GDC0575 hydrochloride
    		Inhibitor
    GDC0575 (ARRY-575) hydrochloride is a highly-selective and orally active Chk1 (IC50=1.2 nM) inhibitor. GDC0575 (ARRY-575) hydrochloride can be used for colitis-associated cancer (CAC) and colitis research.
    GDC0575 hydrochloride
  • HY-P5961
    Chktide
    Chktide is a substrate for CHK1 and CHK2. Chktide can be used in kinase assays.
    Chktide
  • HY-110331
    CCT241533 dihydrochloride
    		Inhibitor
    CCT241533 dihydrochloride is a potent and selective ATP competitive inhibitor of CHK2 with an IC50 of 3 nM and Ki of 1.16 nM.
    CCT241533 dihydrochloride
  • HY-139901
    Chk1-IN-6
    		Inhibitor
    Chk1-IN-6 is a potent, selective, and orally bioavailable CHK1 inhibitor candidate.
    Chk1-IN-6
  • HY-125203
    PV-1019
    		Inhibitor
    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-156470
    Multi-kinase-IN-6
    		Inhibitor
    Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC50 values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect.
    Multi-kinase-IN-6
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Checkpoint Kinase (Chk) Isoform Comparison

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