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-18174
    Prexasertib
    		Inhibitor 99.64%
    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
  • HY-10992
    AZD-7762
    		Inhibitor 99.94%
    AZD-7762 is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC50 of 5 nM for Chk1.
    AZD-7762
  • HY-14720
    Rabusertib
    		Inhibitor 99.98%
    Rabusertib (LY2603618) is a potent and selective inhibitor of Chk1 with an IC50 of 7 nM.
    Rabusertib
  • HY-P99032
    Monalizumab
    		Inhibitor 99.69%
    Monalizumab (IPH2201) is an immune checkpoint inhibitor targeting Natural Killer Group 2A (NKG2A). Monalizumab, a humanized anti-NKG2A blocking mAb, increases IFN-γ production, thereby promoting NK cell effector functions. Monalizumab can be used for the research of head and neck squamous cell carcinoma (HNSCC).
    Monalizumab
  • HY-13946
    BML-277
    		Inhibitor 99.67%
    BML-277 is a selective checkpoint kinase 2 (Chk2) inhibitor with an IC50 of 15 nM.
    BML-277
  • HY-112347
    Isogranulatimide
    		Inhibitor
    Isogranulatimide is a selective checkpoint kinase 1 (Chk1) inhibitor with an IC50 value of 0.1 μM. Isogranulatimide inhibits the G2/M checkpoint and inhibits the growth of p53-mutant tumor cells. Isogranulatimide is promising for research of tumors associated with DNA damage response.
    Isogranulatimide
  • HY-179158
    CHK1-IN-15
    		Ligand
    CHK1-IN-15 (compound 9a) is a ATP-kompetitive inhibitor of Checkpoint-Kinase-1 (CHK1) with a 95% binding at 1.0 µM. CHK1-IN-15 is a Chk1 target protein ligand of MA203 (HY-179157). CHK1-IN-15 can be used in cancer-related research.
    CHK1-IN-15
  • HY-186085
    BEN-28010
    		Inhibitor
    BEN-28010 is a selective, orally active, blood-brain barrier permeable CHK1 inhibitor with an IC50 of 4.0 nM. BEN-28010 functions as a radiosensitizer, exhibits antitumor efficacy in GBM models. BEN-28010 can be used for the research of glioblastoma.
    BEN-28010
  • HY-18958
    CCT245737
    		Inhibitor 99.48%
    CCT245737 (SRA737) is an orally active and seletive Chk1 inhibitor, with an IC50 of 1.3 nM.
    CCT245737
  • HY-15532
    SCH900776
    		Inhibitor 99.97%
    SCH900776 (MK-8776) is a potent, selective and orally bioavailable inhibitor of checkpoint kinase1 (Chk1) with an IC50 of 3 nM. SCH900776 shows 50- and 500-fold selectivity over CDK2 and Chk2, respectively.
    SCH900776
  • HY-157941
    ART0380
    		Inhibitor 99.90%
    ART0380 is a potent, selective and orally active ATR kinase inhibitor. ART0380 potently inhibits human ATR-ATRIP complex with an IC50 of 51.7 nM. ART0380 binds the ATP pocket of the ATR-ATRIP complex, blocks ATR-dependent Chk1 serine 345 phosphorylation, and induces cell cycle disorder and DNA damage. ART0380 demonstrates potent and selective antitumor activity in preclinical models with varying types of ataxia-telangiectasia mutated (ATM) gene aberrancy. ART0380 can be used for the research of cancer, such as colorectal cancer and prostate cancer.
    ART0380
  • HY-13263
    CHIR-124
    		Inhibitor 99.05%
    CHIR-124 is a potent and selective Chk1 inhibitor with IC50 of 0.3 nM, and also potently targets PDGFR and FLT3 with IC50s of 6.6 nM and 5.8 nM.
    CHIR-124
  • HY-14715B
    CCT241533 hydrochloride
    		Inhibitor 98.55%
    CCT241533 hydrochloride is a potent and selective CHK2 inhibitor with an IC50 of 3 nM and a Ki of 1.16 nM.
    CCT241533 hydrochloride
  • HY-10032
    PF 477736
    		Inhibitor 99.04%
    PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, it is also a Chk2 inhibitor, with a Ki of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC50=8 (Ki), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo.
    PF 477736
  • HY-N0245
    Theaflavin-3-gallate
    		99.89%
    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
  • HY-18174A
    Prexasertib dihydrochloride
    		Inhibitor 99.73%
    Prexasertib dihydrochloride (LY2606368 dihydrochloride) 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 dihydrochloride inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dihydrochloride causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dihydrochloride shows potent anti-tumor activity.
    Prexasertib dihydrochloride
  • HY-18961
    PD 407824
    		Inhibitor 99.00%
    PD 407824 is a checkpoint kinase Chk1 and WEE1 inhibitor with IC50s of 47 and 97 nM, respectively. PD 407824 is a chemical BMP sensitizer and increases the sensitivity of cells to sub-threshold amounts of BMP4.
    PD 407824
  • HY-107407
    SB-218078
    		Inhibitor 98.30%
    SB-218078 is a potent, selective, ATP-competitive and cell-permeable checkpoint kinase 1 (Chk1) inhibitor that inhibits Chk1 phosphorylation of cdc25C with an IC50 of 15 nM. SB-218078 is less potently inhibits Cdc2 (IC50 of 250 nM) and PKC (IC50 of 1000 nM). SB-218078 causes apoptosis by DNA damage and cell cycle arrest.
    SB-218078
  • HY-18174E
    Prexasertib dimesylate
    		Inhibitor 98.90%
    Prexasertib dimesylate (LY2606368 dimesylate) 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 dimesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dimesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dimesylate shows potent anti-tumor activity.
    Prexasertib dimesylate
  • HY-148962
    LY2880070
    		Inhibitor 99.9%
    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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Checkpoint Kinase (Chk) Isoform Comparison

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