Checkpoint control kinases is a term used to describe a group of enzymes that regulate progression of a cell through the cell cycle. Catastrophic genetic damage can occur if cells progress to the next phase of the cell cycle before the previous phase is properly completed.
Inhibitors |
Cat. No. | Product Name / Activity |
---|---|
5198 | AZ 20 |
Potent and selective ATR kinase inhibitor; antitumor | |
3994 | AZ 3146 |
Potent and selective Mps1 inhibitor | |
6330 | AZ 5704 |
Potent and selective ATM kinase inhibitor; orally bioavailable. | |
5199 | AZD 7762 hydrochloride |
Potent and selective ATP-competitive inhibitor of Chk1 and Chk2 | |
4968 | CCT 241533 dihydrochloride |
Potent Chk2 inhibitor | |
3271 | Compound 401 |
Selective DNA-PK and mTOR inhibitor | |
4840 | KU 0060648 |
Dual DNA-PK and PI 3-K inhibitor | |
3544 | KU 55933 |
Potent and selective ATM kinase inhibitor | |
6454 | LY 2603618 |
Potent and selective Chk1 inhibitor | |
3190 | Mirin |
MRN-ATM pathway inhibitor | |
5142 | Mps1-IN-1 dihydrochloride |
Selective Mps1 kinase inhibitor | |
3034 | NSC 109555 ditosylate |
Selective Chk2 inhibitor | |
2828 | NU 7026 |
Selective DNA-PK inhibitor | |
3712 | NU 7441 |
Potent and selective DNA-PK inhibitor | |
3785 | PD 166285 dihydrochloride |
Wee1 inhibitor; also inhibits Src, FGFR and PDGFRβ | |
2694 | PD 407824 |
Potent and selective inhibitor of Chk1 and Wee1 | |
4277 | PF 477736 |
Selective Chk1 inhibitor | |
2930 | PI 103 hydrochloride |
Inhibitor of DNA-PK, mTOR and PI 3-kinase | |
2560 | SB 218078 |
Chk1 inhibitor | |
4750 | TC Mps1 12 |
Potent and selective Mps1 kinase inhibitor; orally active | |
3038 | TCS 2312 |
Potent Chk1 inhibitor | |
Other |
Cat. No. | Product Name / Activity |
4502 | DIM |
Activates Chk2; induces G2/M cell cycle arrest | |
4763 | Pyridostatin pentahydrochloride |
Stabilizes G-quadruplexes; induces DNA damage and cell cycle arrest |
Checkpoint control kinases is a term used to describe a group of enzymes that regulate progression of a cell through the cell cycle. Catastrophic genetic damage can occur if cells progress to the next phase of the cell cycle before the previous phase is properly completed. Checkpoint control kinases function to halt the cell cycle at these critical points. Examples of checkpoint control kinases include ATM, ATR, DNA-PK, Chk1, Chk2, Wee1 and mTOR.
For a cell to progress through the cycle and replicate, it must pass through checkpoints between phases to ensure that DNA is replicated correctly and that chromosomes segregate. These checkpoints may stop the cell cycle after DNA damage, loss of DNA replication or disruption of the mitotic spindle, in order for repair processes to take place. If cells containing damaged DNA were to divide, the errors would be transmitted to daughter cells, generating genomic instability and resulting in tumorigenesis or apoptosis.
Tocris offers the following scientific literature for Checkpoint Control Kinases to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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.
Gene | Species | Gene Symbol | Gene Accession No. | Protein Accession No. |
---|---|---|---|---|
ATM | Human | ATM | NM_000051 | Q13315 |
Mouse | Atm | NM_007499 | Q62388 | |
Rat | Atm | NM_001106821 | NP_001100291 | |
ATR | Human | ATR | NM_001184 | Q13535 |
Mouse | Atr | NM_019864 | Q9JKK8 | |
Rat | Atr | XM_236563 | - | |
DNA-PK | Human | PRKDC | NM_001081640 | Q9UME3 |
Mouse | Prkdc | NM_011159 | P97313 | |
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 | |
Wee1 | Human | WEE1 | NM_003390 | P30291 |
Mouse | Wee1 | NM_009516 | P47810 | |
Rat | Wee1 | NM_001012742 | Q63802 | |
mTOR | Human | FRAP1 | NM_004958 | P42345 |
Mouse | Frap1 | NM_020009 | Q9JLN9 | |
Rat | Frap1 | NM_019906 | P42346 |