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Category: EnzymesarrowKinasesarrowBroad Spectrum Protein Kinase Inhibitors
Cat.No. Product Name
1683 K 252a
Alternative name(s): SF 2370
Price and Availability

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K 252a
Chemical Name: (9S,10R,12R)-2,3,9,10,11,12-Hexahydro-10-hydroxy-9-meth yl-1-oxo-9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]py rrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid methyl ester

Biological Activity:

Non-selective protein kinase inhibitor; analogue of staurosporine. 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:

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M.Wt: 467.48
Formula: C27H21N3O5
Storage: Desiccate at -20°C
Solubility: Soluble to 25 mM in DMSO
Purity: >97%
CAS No: [99533-80-9]

Resources:

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    • Certificate of Analysis / MSDS:

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    Product/Material Safety Data Sheet: View current batch

    References:

    Kase et al (1986) K-252a, a potent inhibitor of protein kinase C from microbial origin. J.Antibiot. 39 1059. Ruegg and Burgess (1989) Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases. TiPS 10 218. Knusel and Hefti (1992) K-252 compounds: modulators of neurotrophin signal transduction. J.Neurochem. 59 1987. Morotti et al (2002) K252a inhibits the oncogenic properties of Met, the HGF receptor. Oncogene 21 4885.
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    Keywords: K 252a, Kinases, Protein Kinase Inhibitor, SF 2370, K252a, Tocris Bioscience
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