Biological Activity
Non-selective protein kinase inhibitor; analog of staurosporine (Cat.No. 1285). Inhibits PKC (IC50 = 32.9 nM), Ca2+/calmodulin-stimulated phosphodiesterases (IC50 = 1.3 - 2.9 μM), MLCK (Ki = 20 nM) and receptor tyrosine kinases. Inhibits the oncogenic properties of MET; prevents autophosphorylation and activation of downstream effectors (MAPK, Akt).
Technical Data
| M. Wt | 467.48 |
| Formula | C27H21N3O5 |
| Storage | Desiccate at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 99533-80-9 |
| PubChem ID | 3035817 |
| InChI Key | KOZFSFOOLUUIGY-SOLYNIJKSA-N |
| Smiles | [H][C@](C[C@]8(O)[C@@](OC)=O)(O[C@]78C)N5C3=C2N7C1=CC=CC=C1C2=C(CNC6=O)C6=C3C4=CC=CC=C45 |
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 | 11.69 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 467.48. 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 | 2.14 mL | 10.7 mL | 21.39 mL |
| 5 mM | 0.43 mL | 2.14 mL | 4.28 mL |
| 10 mM | 0.21 mL | 1.07 mL | 2.14 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.43 mL |
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References
References are publications that support the products' biological activity.
Kase et al (1986) K-252a, a potent inhibitor of protein kinase C from microbial origin. J.Antibiot. 39 1059 PMID: 3759657
Knusel and Hefti (1992) K-252 compounds: modulators of neurotrophin signal transduction. J.Neurochem. 59 1987 PMID: 1431889
Morotti et al (2002) K252a inhibits the oncogenic properties of Met, the HGF receptor. Oncogene 21 4885 PMID: 12118367
Ruegg and Burgess (1989) Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases. TiPS 10 218 PMID: 2672462
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