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-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
  • 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
  • HY-124122
    BPTQ
    		Inhibitor
    BPTQ is a potent inhibitor against VEGFR1 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-16129A
    CBP-501 acetate
    		Inhibitor 99.75%
    CBP-501 acetate, a cell-permeable calmodulin-binding peptide and a G2-abrogating drug candidate, inhibits the activity of multiple Ser216-specific kinases, such as MAPKAP-K2, C-Tak1, CHK1 and CHK2, with IC50 values of 0.9 μM, 1.4 μM 3.4 μM and 6.5 μM, respectively. CBP-501 acetate is used for various types of cancer.
    CBP-501 acetate
  • HY-178940
    Apoptosis inducer 49
    		Activator
    Apoptosis inducer 49 is a selective apoptosis inducer with high specificity against CCRF-CEM leukemia cells (IC50 = 2.68 μM). Apoptosis inducer 49 enhances RNA synthesis and replication stress, activates the Chk1-p21 axis, leading to S-phase arrest. Apoptosis inducer 49 can inhibit Bcl-2 and activate caspase-3. Apoptosis inducer 49 can be used for the study of Leukemia.
    Apoptosis inducer 49
  • HY-N0245R
    Theaflavin-3-gallate (Standard)
    Theaflavin-3-gallate (Standard) is the analytical standard of Theaflavin-3-gallate. This product is intended for research and analytical applications. Theaflavin-3-gallate, a black tea theaflavin monomer, is regarded as the biologically important active component of black tea and provides health benefits. Theaflavin-3-gallate acts as prooxidants and induces oxidative stress in the carcinoma cells. Theaflavin-3-gallate reacts directly with reduced glutathione (GSH) in a time- and concentration-dependent manner. Theaflavin-3-gallate induces apoptosis and G1 cell cycle arrest in ovarian cancer A2780/CP70 cells through p53-dependent pathways. Theaflavin-3-gallate induces DNA damage through ATM/Chk/p53 pathway.
    Theaflavin-3-gallate (Standard)
  • HY-179157
    MA203
    		Degrader
    MA203 is a highly efficient and selective PROTAC degrader targeting CHK1. MA203 accelerates CRBN-dependent proteasomal degradation of CHK1 in solid tumor-derived cells and acute leukemia cells. MA203 induces DNA replication stress. MA203 blocks cell cycle progression and triggers tumor cell apoptosis. MA203 does not damage healthy differentiated and primitive hematopoietic cells, stromal cells, and retinal epithelial cells. MA203 can be used for the study of CHK1-dependent cancers.
    MA203
  • 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-103366
    NSC 109555 ditosylate
    		Inhibitor
    NSC 109555 ditosylate is a potent, selective, ATP-competitive checkpoint kinase 2 (Chk2) inhibitor with an IC50 of 240 nM. NSC 109555 ditosylate can be used for the research of cancer.
    NSC 109555 ditosylate
  • 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
  • HY-P991058
    Zimistobart
    		Inhibitor
    Zimistobart (BMS-986315) is a fully human IgG1 antibody that targets NKG2A. Zimistobart can be used for the study of non-small cell lung cancer (NSCLC). The isotype control for Zimistobart can refer to Human IgG1 kappa, Isotype Control (HY-P99001).
    Zimistobart
  • 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-161383
    CHK1-IN-9
    		Inhibitor
    CHK1-IN-9 (compound 11) is an orally active CHK1 inhibitor with an IC50 value of 0.55 nM. CHK1-IN-9 can enhance the effect of DNA-damaging drugs on tumor cells. CHK1-IN-9 has synergistic anticancer effects with Gemcitabine (HY-17026).
    CHK1-IN-9
  • HY-177027
    CHK1-IN-13
    		Inhibitor
    CHK1-IN-13 (Compound 38) is a checkpoint kinase 1 (Chk1) inhibitor with an IC50 of 10-50  nM. CHK1-IN-13 has anticancer activity, and can be used for the research of cancers, such as breast, ovarian and prostate cancer.
    CHK1-IN-13
  • HY-18174S
    Prexasertib-d4
    		Inhibitor
    Prexasertib-d4 (LY2606368-d4) is the deuterium labeled Prexasertib (HY-18174). Prexasertib (LY2606368) 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 inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib shows potent anti-tumor activity.
    Prexasertib-d<sub>4</sub>
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Checkpoint Kinase (Chk) Isoform Comparison

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