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 / Product Datasheet / Safety Data Sheet

Certificate of Analysis / Product Datasheet
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Morotti et al (2002) K252a inhibits the oncogenic properties of Met, the HGF receptor. Oncogene 21 4885. PMID: 12118367.

Knusel and Hefti (1992) K-252 compounds: modulators of neurotrophin signal transduction. J.Neurochem. 59 1987. PMID: 1431889.

Ruegg and Burgess (1989) Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases. TiPS 10 218. PMID: 2672462.

Kase et al (1986) K-252a, a potent inhibitor of protein kinase C from microbial origin. J.Antibiot. 39 1059. PMID: 3759657.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for K 252a include:

Kummer and Cohen (2015) Exercise-induced neuroprotection in the spastic Han Wistar rat: the possible role of brain-derived neurotrophic factor. Neuropsychopharmacology 2015 834543. PMID: 25710032.

Pandya and Pillai (2014) TrkB interacts with ErbB4 and regulates NRG1-induced NR2B phosphorylation in cortical neurons before synaptogenesis. Biomed Res Int 12 47. PMID: 25052836.

Schubert et al (2014) Paraneoplastic CDR2 and CDR2L antibodies affect Purkinje cell calcium homeostasis. Acta Neuropathol 128 835. PMID: 25341622.

Park et al (2013) Inactivation of JAK2/STAT3 signaling axis and downregulation of M1 mAChR cause cognitive impairment in klotho mutant mice, a genetic model of aging. Mol Cells 38 1426. PMID: 23389690.

Meitzen et al (2011) β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons. J Neurochem 116 984. PMID: 21143600.

Do you know of a great paper that uses K 252a from Tocris? If so please let us know.show all ▼show less ▲

Keywords: K 252a, supplier, Protein, kinase, inhibitor, kinases, inhibitors, receptor, tyrosine, inhibits, cMET, HGF, K252a, SF2370, Tocris Bioscience, Broad Spectrum Protein Kinase Inhibitor Inhibitor products

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