Biological Activity
Selective non-lipid inhibitor of sphingosine kinase (IC50 = 0.5 μM); does not act at ATP-binding site. Displays no inhibition of ERK2, PI 3-kinase, or PKCα at concentrations up to 60 μM. Reduces levels of sphingosine-1-phosphate in MDA-MB-231 breast cancer cells. Induces apoptosis and inhibits proliferation in several other tumor cell lines in vitro (IC50 = 0.9 - 4.6 μM).
Technical Data
| M. Wt | 302.78 |
| Formula | C15H11ClN2OS |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 312636-16-1 |
| PubChem ID | 753704 |
| InChI Key | ZFGXZJKLOFCECI-UHFFFAOYSA-N |
| Smiles | OC1=CC=C(NC2=NC(=CS2)C2=CC=C(Cl)C=C2)C=C1 |
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 | 30.28 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 302.78. 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 | 3.3 mL | 16.51 mL | 33.03 mL |
| 5 mM | 0.66 mL | 3.3 mL | 6.61 mL |
| 10 mM | 0.33 mL | 1.65 mL | 3.3 mL |
| 50 mM | 0.07 mL | 0.33 mL | 0.66 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
French et al (2006) Antitumor activity of sphingosine kinase inhibitors. J.Pharmacol.Exp.Ther. 318 596 PMID: 16632640
French et al (2003) Discovery and evaluation of inhibitors of human sphingosine kinase. Cancer Res. 63 5862 PMID:
Keywords: SKI II, supplier, Selective, non-lipid, inhibitors, inhibits, sphingosine, kinases, antitumor, Lipid, Metabolism, sphingosine-1-phosphate, S1P, SKIII, sphk, Sphingosine, Kinase, Sphingosine, Kinase, Tocris Bioscience
