In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
CGK733 is an inhibitor of kinase ATM and ATR with IC50 value of ~200 nM .
Ataxia telangiectasia mutated (ATM) is a serine/threonine kinase which plays pivotal role in DNA repair and cell cycle checkpoints. And when in hypoxia circumstance, loss of ATM-related (ATR) kinase induces the decreasing of HIF-1 DNA binding, which consequently affects GLUT-1 and CAIX expression in the protein level. The components of ATM and ATR regulated signaling pathways which enhances cellular sensitivity to chemo- and radiotherapy thus provide attractive pharmacological targets [2, 3].
CGK733 selectively inhibited ATM and ATR kinase activities and blocked their checkpoint signaling pathways. Treated HEK-293 cells with GSK733 would increase the sensitivity of cells to radiotherapy . When tested with HBV-positive HCC cell line HepG2.2.15, CGK733 treatment significantly increased the cells sensitivity to taxol via inducing the formation of multinucleated cells . Treated with CGK733, senescent breast, lung, and colon carcinoma cells were induced to undergo cell death . CGK733 treated tumor cells could enhance the sensitivity to radio therapy via inhibiting DNA repair and cell cycle checkpoints of tumor cells . In MCF-7 breast cancer cells, CGK733 treatment induced detectable decline levels of cyclin D1 protein and reduced phosphorylated and total retinoblastoma protein (RB) which inhibited cell proliferation .
. Williams, T.M., et al., Molecular imaging of the ATM kinase activity. Int J Radiat Oncol Biol Phys, 2013. 86(5): p. 969-77.
. Wang, H., et al., CGK733 enhances multinucleated cell formation and cytotoxicity induced by taxol in Chk1-deficient HBV-positive hepatocellular carcinoma cells. Biochem Biophys Res Commun, 2012. 422(1): p. 103-8.
. Alao, J.P. and P. Sunnerhagen, The ATM and ATR inhibitors CGK733 and caffeine suppress cyclin D1 levels and inhibit cell proliferation. Radiat Oncol, 2009. 4(51): p. 4-51.
. Crescenzi, E., et al., Ataxia telangiectasia mutated and p21CIP1 modulate cell survival of drug-induced senescent tumor cells: implications for chemotherapy. Clin Cancer Res, 2008. 14(6): p. 1877-87.
. Kuroda, S., Y. Urata, and T. Fujiwara, Ataxia-telangiectasia mutated and the Mre11-Rad50-NBS1 complex: promising targets for radiosensitization. Acta Med Okayama, 2012. 66(2): p. 83-92.
|Physical Appearance||A solid|
|Storage||Store at -20°C|
|Solubility||≥27.8 mg/mL in DMSO; insoluble in H2O; ≥5.55 mg/mL in EtOH with gentle warming and ultrasonic|
|Shipping Condition||Evaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.|
|General tips||For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.|
|Description||CGK 733 is a potent and selective inhibitor of ATM/ATR with an IC50 value of ~200 nM.|
|IC50||200 nM||200 nM|
Quality Control & MSDS
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