Chemical Name: 4,4'-diacetyldiphenylurea bis(guanylhydrazone) ditosylate
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
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.
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.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
7.53
10
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
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Byczkowskiet al (1981) Actions of bis(guanylhydrazones) on isolated rat liver mitochondria. Biochem.Pharmacol. 30 2851 PMID: 6895596
Byczkowskiet al (1982) Potentiation of the antimitochondrial and antiproliferative effects of bis(guanylhydrazones) by phenethylbiguanide. Cancer Res. 42 3592 PMID: 6896674
Jobsonet 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