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.
Technical Data
| M. Wt | 752.86 |
| Formula | C19H24N10O.2C7H8O3S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 66748-43-4 |
| PubChem ID | 12449850 |
| InChI Key | DIQGNVANOSOABS-XMDRLFCYSA-N |
| Smiles | O=C(NC2=CC=C(/C(C)=N/NC(N)=N)C=C2)NC1=CC=C(/C(C)=N/NC(N)=N)C=C1.CC3=CC=C(S(=O)(O)=O)C=C3.CC4=CC=C(S(=O)(O)=O)C=C4 |
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
References
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
Keywords: NSC 109555 ditosylate, supplier, Selective, Chk2, inhibitors, inhibits, Checkpoint, Kinases, Control, NSC109555, ditosylate, DDUG, Checkpoint, Kinases, Checkpoint, Control, Kinases, Checkpoint, Kinases, Tocris Bioscience
