Catalog Number: 1683
Alternate Names: 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.
Background References
  1. K-252a, a potent inhibitor of protein kinase C from microbial origin.
    Kase et al.
    J.Antibiot., 1986;39:1059
  2. K-252 compounds: modulators of neurotrophin signal transduction.
    Knusel and Hefti
    J.Neurochem., 1992;59:1987
  3. Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases.
    Ruegg and Burgess
    TiPS, 1989;10:218
  4. K252a inhibits the oncogenic properties of Met, the HGF receptor.
    Morotti et al.
    Oncogene, 2002;21:4885
Citations:

The citations listed below are publications that use Tocris products. Selected citations for K 252a include:

5 Citations: Showing 1 - 5
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  1. Exercise-induced neuroprotection in the spastic Han Wistar rat: the possible role of brain-derived neurotrophic factor.
    Authors: Kummer and Cohen
    Neuropsychopharmacology 2015;2015:834543
  2. TrkB interacts with ErbB4 and regulates NRG1-induced NR2B phosphorylation in cortical neurons before synaptogenesis.
    Authors: Pandya and Pillai
    Biomed Res Int 2014;12:47
  3. Paraneoplastic CDR2 and CDR2L antibodies affect Purkinje cell calcium homeostasis.
    Authors: Schubert Et al.
    Acta Neuropathol 2014;128:835
  4. Inactivation of JAK2/STAT3 signaling axis and downregulation of M1 mAChR cause cognitive impairment in klotho mutant mice, a genetic model of aging.
    Authors: Park Et al.
    Mol Cells 2013;38:1426
  5. β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons.
    Authors: Meitzen Et al.
    J Neurochem 2011;116:984

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