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.
All Tocris products are intended for laboratory research use only.

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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