Cat. No. 1683
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 ActivityNon-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).
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
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.
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Keywords: K 252a, supplier, Protein, kinase, inhibitor, kinases, inhibitors, receptor, tyrosine, inhibits, cMET, HGF, K252a, SF2370
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