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.
Checkpoint Kinase Inhibitors |
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|---|---|
| Cat. No. | Product Name / Activity |
| 7589 | Adavosertib |
| Potent and selective Wee1 inhibitor | |
| 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 | |
Degraders |
|
| Cat. No. | Product Name / Activity |
| 7240 | ZNL 02-096 |
| Potent and selective Wee1 Degrader; arrests cells in the G2/M phase and induces apoptosis | |
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* your copy today!
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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. 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.
Our Cell Cycle & DNA Damage Repair 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.
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