Checkpoint Kinase (Chk)
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
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Checkpoint Kinase (Chk) Inhibitors
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Checkpoint Kinase (Chk) Agonist
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Checkpoint Kinase (Chk) Activators
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Checkpoint Kinase (Chk) Degraders
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Checkpoint Kinase (Chk) Substrates
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Checkpoint Kinase (Chk) Ligands
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Checkpoint Kinase 1 (Chk1) Proteins
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Checkpoint Kinase 2 (Chk2) Proteins
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Checkpoint Kinase (Chk) Related Products (122)
Related Products (122)
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Recombinant Proteins (6)
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Antibodies (10)
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Checkpoint Kinase (Chk) Isoform Comparison
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Chk1-IN-6
0 ImagesChk1-IN-6 is a selective and orally active Chk1 inhibitor with an IC50 of 16.1 nM. Chk1-IN-6 shows antiproliferative activity of MV-4-11 cells. Chk1-IN-6 exerts effective response in the MV-4-11 xenograft mouse model. Chk1-IN-6 exhibits synergistic anticancer effect with Gemcitabine (HY-17026). Chk1-IN-6 can be used in the research of cancers such as acute myeloid leukemia and colorectal adenocarcinoma.
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PROTAC Chk1 degrader-1
0 ImagesPROTAC Chk1 degrader-1 is a Chk1-targeting PROTAC.PROTAC Chk1 degrader-1 recruits the Cereblon E3 ligase to induce ubiquitination and proteasomal degradation of Chk1.PROTAC Chk1 degrader-1 exhibits Chk1 degradation activity in malignant melanoma cells without showing a hook effect.PROTAC Chk1 degrader-1 can be used for the research of malignant melanoma.
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CHEK1 Human Pre-designed siRNA Set A
0 ImagesCat. No.: HY-RS02616CHEK1 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.
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CCT241533
0 ImagesCat. No.: HY-14715CAS No.: 1262849-73-9CCT241533 is a potent and selective ATP competitive inhibitor of CHK2 with an IC50 of 3 nM and Ki of 1.16 nM.
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Prexasertib Mesylate Hydrate
0 ImagesCat. No.: HY-18174BCAS No.: 1234015-57-6Synonyms: LY2606368 Mesylate Hydrate; LY2940930Prexasertib 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.
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CHK1-IN-7
0 ImagesCat. No.: HY-103367CAS No.: 838823-31-7
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Zimistobart
0 ImagesCat. No.: HY-P991058CAS No.: 2829290-06-2Synonyms: BMS-986315
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Prexasertib-d4
0 ImagesCat. No.: HY-18174SSynonyms: LY2606368-d4Prexasertib-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.
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CBP-501
0 ImagesCat. No.: HY-16129CAS No.: 565434-85-7CBP-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.
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BBI-2779
0 ImagesCat. No.: HY-155798CAS No.: 2871057-47-3BBI-2779 is a highly selective, orally active CHK1 inhibitor with a CHK1 IC50 of 0.3 nM. BBI-2779 leverages transcription-replication conflicts on extrachromosomal DNA (ecDNA) to induce synthetic lethality, replication stress, DNA damage and cell death in ecDNA-positive tumor cells. BBI-2779 blocks ecDNA-mediated acquired resistance to targeted therapies and inhibits tumor growth in mouse models of gastric cancer. BBI-2779 is applicable to ecDNA-positive cancer-related research.
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CHK1-IN-4 hydrochloride
0 ImagesCat. No.: HY-128766ACHK1-IN-4 hydrochloride is a selective checkpoint kinase 1 (Chk1) inhibitor with an IC50 ≤ 1 nM. The IC50 value of CHK1-IN-4 hydrochloride against Chk2 ranges from 50 to 100 nM. CHK1-IN-4 hydrochloride inhibits cancer cell proliferation and exhibits antitumor activity in colon cancer xenograft models. CHK1-IN-4 hydrochloride can be used for the research of colon cancer and breast cancer.
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Cyproheptadine hydrochloride sesquihydrate (Standard)
0 ImagesCyproheptadine hydrochloride sesquihydrate (Standard) is the analytical standard of Cyproheptadine hydrochloride sesquihydrate (HY-B1165). This product is intended for research and analytical applications. Cyproheptadine hydrochloride sesquihydrate acts as a p38 MAP kinase activator, CHK2 activator, histamine H1 receptor inhibitor and serotonin receptor inhibitor. Cyproheptadine hydrochloride sesquihydrate mediates cell cycle arrest via G1 phase arrest, G1/S transition arrest, G0/G1 phase arrest, reduced expression of cyclins D1/D2/D3, upregulated expression of HBP1, p16, p21, p27, and decreased phosphorylation of retinoblastoma protein. Cyproheptadine hydrochloride sesquihydrate induces Apoptosis by increasing PARP and cleaved PARP, as well as activating the mitochondrial caspase pathway. Cyproheptadine hydrochloride sesquihydrate inhibits tumor growth with extremely low toxicity to normal cells. Cyproheptadine hydrochloride sesquihydrate can be used in research related to hepatocellular carcinoma, multiple myeloma and acute myeloid leukemia.
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Prexasertib mesylate
0 ImagesCat. No.: HY-18174CCAS No.: 1234015-55-4Synonyms: LY2606368 mesylatePrexasertib 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.
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VER-00158411
0 ImagesCat. No.: HY-18942CAS No.: 1174664-88-0VER-00158411 is a checkpoint kinase 1 (CHK1) and CHK2 inhibitor with IC50 values of 4.4 nM and 4.5 nM, respectively.
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CHK1-IN-2
0 ImagesCat. No.: HY-111369CAS No.: 912367-45-4CHK1-IN-2 is a checkpoint kinase 1 (CHK1) inhibitor, with an IC50 of 6 nM.
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NSC 109555
0 ImagesCat. No.: HY-123597CAS No.: 15427-93-7Synonyms: DDUG; NCI C04808NSC 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.
