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  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-128766A
    CHK1-IN-4 hydrochloride
    		Inhibitor
    CHK1-IN-4 hydrochloride (Compound 3) is a potent checkpoint kinase 1 (chk1) inhibitor, and potently inhibits chk1 phosphorylation in the tumor cells. CHK1-IN-4 hydrochloride has anti-tumor activity.
    CHK1-IN-4 hydrochloride
  • 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-18942
    VER-00158411
    		Inhibitor
    VER-00158411 is a checkpoint kinase 1 (CHK1) and CHK2 inhibitor with IC50 values of 4.4 nM and 4.5 nM, respectively.
    VER-00158411
  • 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-123597
    NSC 109555
    		Inhibitor
    NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50=200 nM in a cell-free kinase assay). It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50=240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.2 NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.
    NSC 109555
  • 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-RS02618
    Chek1 Rat Pre-designed siRNA Set A
    		Inhibitor

    Chek1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Chek1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Chek1 Rat Pre-designed siRNA Set A
    Chek1 Rat Pre-designed siRNA Set A
  • HY-158303
    Chk2-IN-2
    		Inhibitor
    Chk2-IN-2 (compound 2) is a selective inhibitor of CHK2 with potential anticancer activity.
    Chk2-IN-2
  • HY-161622
    K1586
    		Inhibitor
    K1586 is an amidine derivative that efficiently targets Chk1. K1586 enhances the degradation of Chk1 that sensitizes colorectal cancer cells to ionizing radiation. K1586 shows anticancer effects.
    K1586
  • HY-RS02619
    CHEK2 Human Pre-designed siRNA Set A
    		Inhibitor

    CHEK2 Human Pre-designed siRNA Set A contains three designed siRNAs for CHEK2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    CHEK2 Human Pre-designed siRNA Set A
    CHEK2 Human Pre-designed siRNA Set A
  • HY-P10367
    Ziptide
    Ziptide is a substrate for MAPK activated protein kinase 2 (MAPKAPK2, Km = 5 μM), MAPKAPK3 (Km = 30 μM), PARK (Km = 40 μM), checkpoint kinase 1 (Chk1, Km = 5 μM), AMP-activated protein kinase (AMPK, Km = 75 μM), and calcium/calmodulin-dependent protein kinase II (CamKII, Km = 300 μM).
    Ziptide
  • HY-RS02620
    Chek2 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Chek2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Chek2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Chek2 Mouse Pre-designed siRNA Set A
    Chek2 Mouse Pre-designed siRNA Set A
  • HY-RS02621
    Chek2 Rat Pre-designed siRNA Set A
    		Inhibitor

    Chek2 Rat Pre-designed siRNA Set A contains three designed siRNAs for Chek2 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Chek2 Rat Pre-designed siRNA Set A
    Chek2 Rat Pre-designed siRNA Set A
  • HY-124122
    BPTQ
    		Inhibitor
    BPTQ is a potent inhibitor against VEGFR1/Flt-1 and CHK2 with IC50 values of 0.54 and 1.70 µmol/L, respectively. BPTQ is also an intercalator of DNA with anticancer activities. BPTQ inhibits the proliferation of HL-60 cells by arresting cells at S and G2/M phase with an IC50 value of 12 µmol/L. BPTQ also activates the mitochondria-mediated Apoptosis pathway by a decrease in mitochondrial membrane potential, increase in the Bax:Bcl-2 ratio and activation of caspases.
    BPTQ
  • 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-162367
    FLT3/CHK1-IN-2
    		Inhibitor
    FLT3/CHK1-IN-2 (Compound 30) is a dual inhibitor of FLT3 and CHK1, with IC50s of 25.63, 16.39, 22.80 nM for CHK1, FLT3-WT, and FLT-D835Y respectively. FLT3/CHK1-IN-2 has favorable oral PK properties and kinase selectivity. FLT3/CHK1-IN-2 can be used for research of acute myeloid leukemia (AML).
    FLT3/CHK1-IN-2
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Checkpoint Kinase (Chk) Isoform Comparison

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