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

Checkpoint Kinase (Chk)

Checkpoint Kinase (Chk)

Related Products

PDF 0.16 MB

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-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-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-112927
    MU380
    		Inhibitor 99.6%
    MU380 is a potent and selective CHK1 inhibitor that induces apoptosis and has anticancer activity.
    MU380
  • HY-47026
    Protein kinase inhibitor 6
    		Inhibitor 99.04%
    Protein kinase inhibitor 6 is a protein kinase inhibitor.
    Protein kinase inhibitor 6
  • HY-16129
    CBP-501
    		Inhibitor 99.75%
    CBP-501, 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 is used for various types of cancer.
    CBP-501
  • 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 is a selective and ATP-competitive Chk2 inhibitor with an IC50 of 120 nM and a Ki of 11 nM. VRX0466617 does not inhibit the related Chk1 activity. 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
  • 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-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
  • HY-119699
    PV1115
    		Inhibitor
    PV1115 is a potent and highly selective Chk2 inhibitor with an IC50 of 0.14 nM, 66000 nM, >100000 nM for Chk2, Chk1 and RSK2, respectively. PV1115 is situated within the ATP-binding pocket of Chk2.
    PV1115
  • HY-124731
    PD-321852
    		Inhibitor
    PD-321852 is a Chk1 inhibitor, with IC50 of 5 nM. PD-321852 can be used in anti-cancer research.
    PD-321852
  • 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-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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Checkpoint Kinase (Chk) Isoform Comparison

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.