NSC 109555 ditosylate
Selective, reversible, ATP-competitive Chk2 inhibitor (IC50 = 0.2 μM) that displays no effect on a range of other kinases including Chk1 (IC50 > 10 μM). Inhibits histone H1 phosphorylation (IC50 = 0.24 μM) and attenuates mitochondrial ATP synthesis. Exhibits antiproliferative activity in a number of leukemias in vivo.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 752.86. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.33 mL||6.64 mL||13.28 mL|
|5 mM||0.27 mL||1.33 mL||2.66 mL|
|10 mM||0.13 mL||0.66 mL||1.33 mL|
|50 mM||0.03 mL||0.13 mL||0.27 mL|
References are publications that support the products' biological activity.
Byczkowski et al (1981) Actions of bis(guanylhydrazones) on isolated rat liver mitochondria. Biochem.Pharmacol. 30 2851 PMID: 6895596
Byczkowski et al (1982) Potentiation of the antimitochondrial and antiproliferative effects of bis(guanylhydrazones) by phenethylbiguanide. Cancer Res. 42 3592 PMID: 6896674
Jobson et al (2007) Identification of a bis-guanylhydrazone [4,4'-diacetyldiphenylurea-bis(guanylhydrazone); NSC 109555] as a novel chemotype for inhibition of Chk2 kinase. Mol.Pharmacol. 72 876 PMID: 17616632
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2 Citations for NSC 109555 ditosylate
Citations are publications that use Tocris products. Selected citations for NSC 109555 ditosylate include:
Fard et al (2013) The heterogenic final cell cycle of chicken retinal Lim1 horizontal cells is not regulated by the DNA damage response pathway. Cell Cycle 13 408 PMID: 24247150
Duong et al (2013) Inhibition of checkpoint kinase 2 (CHK2) enhances sensitivity of pancreatic adenocarcinoma cells to gemcitabine. J Cell Mol Med 17 1261 PMID: 23855452
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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.