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
Gene Data

Inhibitors

Cat No Product Name / Activity
5199 AZD 7762 hydrochloride
Potent and selective ATP-competitive inhibitor of Chk1 and Chk2
4968 CCT 241533 dihydrochloride
Potent Chk2 inhibitor
3034 NSC 109555 ditosylate
Selective Chk2 inhibitor
2694 PD 407824
Selective inhibitor of Chk1 and Wee1
4277 PF 477736
Selective Chk1 inhibitor
2560 SB 218078
Inhibitor of checkpoint kinase 1 (Chk1)
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.

Literature for Checkpoint Kinases

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