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 ActivityK 252a is a 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).
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Tocris products are intended for laboratory research use only, unless stated otherwise.
K-252a, a potent inhibitor of protein kinase C from microbial origin.
Kase et al.
K-252 compounds: modulators of neurotrophin signal transduction.
Knusel and Hefti
K252a inhibits the oncogenic properties of Met, the HGF receptor.
Morotti et al.
Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases.
Ruegg and Burgess
Citations for K 252a
The citations listed below are publications that use Tocris products. Selected citations for K 252a include:
7 Citations: Showing 1 - 7
Aging Increases Hippocampal DUSP2 by a Membrane Cholesterol Loss-Mediated RTK/p38MAPK Activation Mechanism.
Authors: Martín-Segura Et al.
Front Neurol 2019;10:675
Exercise-induced neuroprotection in the spastic Han Wistar rat: the possible role of brain-derived neurotrophic factor.
Authors: Kummer and Cohen
BDNF released during neuropathic pain potentiates NMDA receptors in primary afferent terminals.
Authors: Chen Et al.
Eur J Neurosci 2014;39:1439
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
Paraneoplastic CDR2 and CDR2L antibodies affect Purkinje cell calcium homeostasis.
Authors: Schubert Et al.
Acta Neuropathol 2014;128:835
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
β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons.
Authors: Meitzen Et al.
J Neurochem 2011;116:984
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