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-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-112477A
    (E/Z)-Chk2-IN-1
    		Inhibitor
    (E/Z)-Chk2-IN-1 ((E/Z)-Hymenialdisine analogue-1) (Compound 1) is a potent and selective cell cycle kinase Chk2 inhibitor with an IC50 of 8 nM. (E/Z)-Chk2-IN-1 exhibits low inhibitory activity against other kinases (such as CK1δ, MEK1, and PKCα/βⅡ) with IC50 values both >89 nM. (E/Z)-Chk2-IN-1 can be used for the research of cancer.
    (E/Z)-Chk2-IN-1
  • 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-182016
    PROTAC ATR degrader-3
    		Degrader
    PROTAC ATR degrader-3 is a potent CRBN-based ATR PROTAC degrader with a DC50 of 127 nM. PROTAC ATR degrader-3 also degrades CHK1 with an DC50 of 135 nM. PROTAC ATR degrader-3 inhibits cancer cells proliferation, migration and invasion, triggers apoptosis and induces S phase arrest and DNA damage. PROTAC ATR degrader-3 achieves tumor growth inhibition in LoVo xenograft mouse model without apparent toxicity. PROTAC ATR degrader-3 can be used for the research of colorectal cancer.
    PROTAC ATR degrader-3
  • 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>
  • 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
  • HY-177551
    CHK1-IN-14
    		Inhibitor
    CHK1-IN-14 is a free base form of CHK1 inhibitor. CHK1-IN-14 can be used in research on resistance to chemotherapy and radiotherapy.
    CHK1-IN-14
  • HY-160948
    DB07006
    		Inhibitor
    DB07006 (compound 18) is a potent, ATP-cpmpetitive dual inhibitor of Wee1 (IC50 = 0.030 μM) and Chk1 checkpoint kinases (IC50 = 0.018 μM). DB07006 demonstrates effective abrogation of the G2/M checkpoint in combination with DNA-damaging agents in cellular models. DB07006 can be used for cancer research.
    DB07006
  • HY-18958A
    (S)-CCT245737
    		Inhibitor
    (S)-CCT245737 ((S)-SRA737) is a potent and selective oral inhibitor of checkpoint kinase 1 (CHK1).
    (S)-CCT245737
  • HY-P10574
    Phosphorylated CHKtide
    Phosphorylated CHKtide is a synthetic peptide substrate derived from CDC25C, which is phosphorylated by CHK1/CHK2 in one of the DNA repair pathways. Phosphorylated CHKtide is used in the assays of cell cycle checkpoint kinases 1 and 2 (CHK1/CHK2) and salt-inducible kinases (SIKs).
    Phosphorylated CHKtide
  • HY-178869
    FLT3/CHK1 ligand-1
    		Ligand
    FLT3/CHK1 ligand-1 is a PROTAC target protein ligand that can be used for synthesis of PROTACs, such as PROTAC FLT3/CHK1 Degrader-1 (HY-178858). PROTAC FLT3/CHK1 Degrader-1 is a potent FLT3/CHK1 PROTAC degrader with anti-tumor activity.
    FLT3/CHK1 ligand-1
  • HY-RS02617
    Chek1 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Chek1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Chek1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Chek1 Mouse Pre-designed siRNA Set A
  • HY-178858
    PROTAC FLT3/CHK1 Degrader-1
    		Degrader
    PROTAC FLT3/CHK1 Degrader-1 is a PROTAC FLT3/CHK1 degrader, with DC50 values of 5.88 nM (FLT3) and 4.17 nM (CHK1), respectively. PROTAC FLT3/CHK1 Degrader-1 can inhibit the phosphorylation of FLT3 downstream signaling effectors STAT5 (Tyr694), AKT (Ser473), and ERK (Tyr204), downregulate the protein level of c-Myc and maintain the expression of p53 protein. PROTAC FLT3/CHK1 Degrader-1 induces apoptosis in MV-4-11 cells. PROTAC FLT3/CHK1 Degrader-1 shows significant anti-tumor efficacy in mice bearing MV-4-11 subcutaneous xenografts. PROTAC FLT3/CHK1 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/CHK1 ligand (HY-178869 ), Blue: CRBN Ligand (HY-W093272), Black: Linker, E3 ligase ligand-linker conjugate (HY-W998238)).
    PROTAC FLT3/CHK1 Degrader-1
  • HY-124774
    XL-844
    		Inhibitor
    XL-844 (EXEL-9844) is an inhibitor of Chk1 and Chk2. XL-844 exhibits antineoplastic activity. XL-844 can result in tumor cell apoptosis through inhibition of cell cycle arrest. XL-844 inhibits VEGFR1 and VEGFR3. XL-844 can be studied in anti-cancer research.
    XL-844
  • HY-171785
    CHK1-IN-12
    		Inhibitor
    CHK1-IN-12 (Compound example 1-5) is an orally active and highly selective checkpoint kinase 1 (CHK1) inhibitor with in vitro enzyme IC50≤10 nM and cellular IC50≤50 nM. CHK1-IN-12 inhibits the phosphorylation activity of CHK1 kinase to block the DNA damage response pathway, inducing tumor cell cycle arrest and apoptosis. CHK1-IN-12 is promising for research of cancers.
    CHK1-IN-12
  • HY-155798
    CHK1-IN-8
    		Inhibitor
    CHK1-IN-8 (example 3-2) is a Chk1 inhibitor with an IC50 of <10 nM for human Chk1. CHK1-IN-8 can be used for the study of cancer.
    CHK1-IN-8
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Checkpoint Kinase (Chk) Isoform Comparison

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