R&D Systems Inc. Tocris Bioscience Boston Biochem

K 252a

Cat. No. 1683

K 252a C27H21N3O5 [99533-80-9]

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Alternative Name: SF 2370

Chemical Name: (9S,10R,12R)-2,3,9,10,11,12-Hexahydro-10-hydroxy-9-methyl-1-oxo-9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid methyl ester

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
Solubility:
Soluble to 25 mM in DMSO
Purity:
>98 %
Storage:
Desiccate at -20°C
CAS No:
99533-80-9

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
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Safety Data Sheet: View Safety Data Sheet

References

Kase et al (1986) K-252a, a potent inhibitor of protein kinase C from microbial origin. J.Antibiot. 39 1059. PMID: 3759657.

Ruegg and Burgess (1989) Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases. TiPS 10 218. PMID: 2672462.

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.

If you know of a relevant citation for this product please let us know.

Keywords: K 252a, supplier, Protein, kinase, inhibitor, kinases, inhibitors, receptor, tyrosine, inhibits, cMET, HGF, K252a, SF2370

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