Checkpoint Control Kinases

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.

Products
Background
Literature
Gene Data

Inhibitors

Cat No Product Name / Activity
5198 AZ 20
Potent and selective ATR kinase inhibitor; antitumor
3994 AZ 3146
Potent and selective Mps1 inhibitor
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
2088 DMNB
DNA-PK inhibitor
4840 KU 0060648
Dual DNA-PK and PI 3-K inhibitor
3544 KU 55933
Potent and selective ATM kinase inhibitor
4176 KU 60019
Potent ATM kinase inhibitor
3190 Mirin
MRN-ATM pathway inhibitor
5562 Mps BAY 2a
Potent and selective Mps1 kinase 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
Selective inhibitor of Chk1 and Wee1
4277 PF 477736
Selective Chk1 inhibitor
3140 PHA 767491 hydrochloride
Dual cdc7/cdk9 inhibitor. Also inhibits MK2
2930 PI 103 hydrochloride
Inhibitor of DNA-PK, mTOR and PI 3-kinase
2560 SB 218078
Inhibitor of checkpoint kinase 1 (Chk1)
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.

Literature for Checkpoint Control 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 Control Kinase Gene Data

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