Checkpoint Kinases

Checkpoint kinases (Chks) are serine/threonine kinases that are involved in the control of the cell cycle. Two subtypes have so far been identified, Chk1 and Chk2. They are essential components to delay cell cycle progression in all cells and act at all three cell cycle checkpoints.

Products
Background
Literature (3)
Gene Data

Inhibitors

Cat. No. Product Name / Activity
5199 AZD 7762 hydrochloride
Potent and selective ATP-competitive inhibitor of Chk1 and Chk2; also enhances CRISPR-Cpf1-mediated genome editing
4968 CCT 241533 dihydrochloride
Potent Chk2 inhibitor
6454 LY 2603618
Potent and selective Chk1 inhibitor
3034 NSC 109555 ditosylate
Selective Chk2 inhibitor
2694 PD 407824
Potent and selective inhibitor of Chk1 and Wee1
4277 PF 477736
Selective Chk1 inhibitor
2560 SB 218078
Chk1 inhibitor
3038 TCS 2312
Potent Chk1 inhibitor

Activators

Cat. No. Product Name / Activity
4502 DIM
Activates Chk2; induces G2/M cell cycle arrest

Checkpoint kinases (Chks) are serine/threonine kinases that are involved in the control of the cell cycle. Two subtypes have so far been identified, Chk1 and Chk2. They are essential components to delay cell cycle progression in normal and damaged cells and can act at all three cell cycle checkpoints.

Chks are activated by phosphorylation. ATR kinase phosphorylates Chk1 in response to single strand DNA breaks and ATM kinase phosphorylates Chk2 in response to double strand breaks. Chks phosphorylate Cdc25 phosphatase at Ser216, which leads to Cdc25 sequestration in the cytoplasm. Therefore Cdc25 cannot remove the inhibitory phosphorylation on mitotic promoting factor (MPF) and entry into mitosis is prohibited. In addition, Chks have a role in the physiological stress of hypoxia/reoxygenation.

External sources of pharmacological information for Checkpoint Kinases :

    Literature for Checkpoint Kinases

    Tocris offers the following scientific literature for Checkpoint Kinases to showcase our products. We invite you to request* or download your copy today!

    *Please note that Tocris will only send literature to established scientific business / institute addresses.


    Cancer

    Cancer Research Product Guide

    A collection of over 750 products for cancer research, the guide includes research tools for the study of:

    • Cancer Metabolism
    • Epigenetics in Cancer
    • Receptor Signaling
    • Cell Cycle and DNA Damage Repair
    • Angiogenesis
    • Invasion and Metastasis
    Kinases

    Kinases Product Listing

    A collection of over 400 products for kinase research, the listing includes inhibitors of:

    • Receptor Tyrosine Kinases
    • Protein Kinases A, C, D and G
    • PI-3 Kinase, Akt and mTOR
    • MAPK Signaling
    • Receptor Serine/Threonine Kinases
    Cell Cycle & DNA Damage Repair

    Cell Cycle & DNA Damage Repair Poster

    In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.

    Checkpoint Kinase Gene Data

    Gene Species Gene Symbol Gene Accession No. Protein Accession No.
    Chk1 Human CHEK1 NM_001274 O14757
    Mouse Chek1 NM_007691 O35280
    Rat Chek1 NM_080400 Q91ZN7
    Chk2 Human CHEK2 NM_001005735 O96017
    Mouse Chek2 NM_016681 Q9Z265
    Rat Chek2 NM_053677 Q9R019