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-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 98.01%
    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
  • HY-153857
    Lasmotinib
    		Inhibitor 98.97%
    Lasmotinib (PHI-101) is a FLT3 and CHK2 inhibitor. Lasmotinib potently inhibits FLT3 single activating mutations (ITD or TKD mutants) and has inhibitory activity against FLT3 double (ITD/D835Y or ITD/F691L) and triple (ITD/D835Y/F691L) resistance mutations. Lasmotinib synergizes with Venetoclax (HY-15531) or Azacytidine to inhibit leukemia. Lasmotinib exhibits anticancer activity against ovarian and breast cancer.
    Lasmotinib
  • HY-13649
    Indibulin
    		Activator 99.89%
    Indibulin (ZIO 301), an orally applicable inhibitor of tubulin assembly, shows potent anticancer activity with a minimal neurotoxicity. Indibulin reduces inter-kinetochoric tension, produces aberrant spindles, activates mitotic checkpoint proteins Mad2 and BubR1, and induces mitotic arrest and apoptosis.
    Indibulin
  • HY-19926
    GDC-0425
    		Inhibitor 99.60%
    GDC-0425 (RG-7602) is an orally available, highly selective small molecule ChK1 inhibitor. GDC-0425 can be used for the research of various malignancies.
    GDC-0425
  • HY-112167A
    GDC-0575 dihydrochloride
    		Inhibitor 99.32%
    GDC-0575 dihydrochloride (ARRY-575 dihydrochloride) is an orally bioavailable CHK1 inhibitor, with an IC50 of 1.2 nM, and has antitumor activity.
    GDC-0575 dihydrochloride
  • HY-125203
    PV-1019
    		Inhibitor 99.30%
    PV-1019 (NSC 744039) is a potent, selective Chk2 inhibitor with an IC50 value of 24 nM. PV-1019 inhibits the Topotecan (HY-13768)-induced Chk2 autophosphorylation. PV-1019 inhibits IR-induced apoptosis.
    PV-1019
  • HY-100195
    SAR-020106
    		Inhibitor 98.04%
    SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM for human CHK1. SAR-020106 shows excellent selectivity over CHK2. SAR-020106 significantly enhances the cell killing of Gemcitabine and SN38 by 3- to 29-fold in several colon tumor lines and in a p53-dependent fashion. SAR-020106 can enhance antitumor activity with selected anticancer agents.
    SAR-020106
  • HY-40029
    (S)-1-Boc-3-aminopiperidine
    		99.95%
    (S)-1-Boc-3-aminopiperidine is a key intermediate for the synthesis of various novel inhibitors, such as CHK1 inhibitors and PI3Kδ inhibitors.
    (S)-1-Boc-3-aminopiperidine
  • HY-147228
    NR2F6 modulator-1
    		Modulator 99.46%
    NR2F6 modulator-1 is a potent nuclear receptor subfamily 2, group F, member 6 (NR2F6) modulator. NR2F6 modulator-1 can be used for researching immune modulation and modulation of cancer stem cell activity.
    NR2F6 modulator-1
  • HY-15883
    GNE-900
    		Inhibitor 99.21%
    GNE-900 is a an ATP-competitive, selective, and orally active ChK1 inhibitor with IC50s of 0.0011, 1.5 µM for ChKl, ChK2, respectively. GNE-900 abrogates the G2-M checkpoint, enhances DNA damage, and induces Apoptosis.html" class="link-product" target="_blank">Apoptosis. gemcitabine (HY-17026) and GNE-900 administration shows anti-tumor activity.
    GNE-900
  • HY-122198
    ML367
    		Inhibitor 99.84%
    ML367 is a potent inhibitor of ATPase family AAA domain-containing protein 5 (ATAD5) stabilization, acts as a probe molecule that has low micromolar inhibitory activity. ML367 blocks DNA repair pathways, suppresses general DNA damage responses including RPA32-phosphorylation and CHK1-phosphorylation in response to UV irradiation.
    ML367
  • HY-117857
    MRT00033659
    		Inhibitor 99.77%
    MRT00033659 is a potent broad-spectrum kinase inhibitor of CK1 (IC50=0.9 μM for CK1δ) and CHK1 (IC50=0.23 μM). MRT00033659, a pyrazolo-pyridine analogue, induces p53 pathway activation and E2F-1 destabilisation.
    MRT00033659
  • HY-117102
    ANI-7
    		Activator 99.01%
    ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells, and potently and selectively inhibits the growth of MCF-7 breast cancer cells with a GI50 of 0.56 μM. ANI-7 induces CYP1-metabolizing mono-oxygenases by activating AhR pathway, and also induces DNA damage, checkpoint Kinase 2 (Chk2) activation, S-phase cell cycle arrest, and cell death in sensitive breast cancer cell lines.
    ANI-7
  • HY-128601
    CHK1-IN-3
    		Inhibitor 99.79%
    CHK1-IN-3 is a potent and selective CHK1 inhibitor with an IC50 of 0.4 nM. CHK1-IN-3 effectively inhibits the growth of malignant hematopathy cell lines and displays low affinity for hERG (IC50 > 40 μM). CHK1-IN-3 significantly suppresses the tumor growth in vivo. CHK1-IN-3 can be used for the study of hematologic malignancies.
    CHK1-IN-3
  • HY-19916A
    Lisavanbulin dihydrochloride
    		Activator 99.74%
    Lisavanbulin (BAL-101553) dihydrochloride is the prodrug of the microtubule targeting agent Avanbulin (BAL 27862) (HY-106008). Lisavanbulin dihydrochloride exhibits antitumor activity, especially in tumors that express high levels of end-binding protein 1. Lisavanbulin dihydrochloride has ability to target tumor cell proliferation and affects the tumor microenvironment by reducing tumor microvasculature. Lisavanbulin dihydrochloride is also a spindle assembly checkpoint activator, agonistic anti-CD40 antibody, and double immune checkpoint blockade (anti-PD-1 and anti-CTLA-4). Lisavanbulin dihydrochloride induces cell cycle arrest and subsequent death or aberrant chromosome segregation. Lisavanbulin dihydrochloride can be studied in research for diffuse large B cell lymphoma (DLBCL) and glioblastoma.
    Lisavanbulin dihydrochloride
  • HY-19916
    Lisavanbulin
    		Activator 99.24%
    Lisavanbulin (BAL-101553) is the prodrug of the microtubule targeting agent Avanbulin (BAL 27862) (HY-106008). Lisavanbulin is a BBB-penetrant and orally active antitumor agent, especially in tumors that express high levels of end-binding protein 1. Lisavanbulin has ability to target tumor cell proliferation and affects the tumor microenvironment by reducing tumor microvasculature. Lisavanbulin is also a spindle assembly checkpoint activator, agonistic anti-CD40 antibody, and double immune checkpoint blockade (anti-PD-1 and anti-CTLA-4). Lisavanbulin induces cell cycle arrest and subsequent death or aberrant chromosome segregation. Lisavanbulin can be studied in research for diffuse large B cell lymphoma (DLBCL) and glioblastoma.
    Lisavanbulin
  • HY-103367
    CHK1-IN-7
    		Inhibitor ≥98.0%
    CHK1-IN-7 (Compound 10c) is a potent human CHK1 inhibitor. CHK1-IN-7 shows no single agent effect, potentiates the antiproliferative effect of Gemcitabine HY-17026 in both prostate and breast cancer cell lines. CHK1-IN-7 can be used for the research of cancer.
    CHK1-IN-7
  • HY-10992A
    AZD-7762 hydrochloride
    		Inhibitor 99.58%
    AZD-7762 hydrochloride is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC50 of 5 nM for Chk1.
    AZD-7762 hydrochloride
  • HY-131446
    Chk1-IN-5
    		Inhibitor 98.84%
    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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Checkpoint Kinase (Chk) Isoform Comparison

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