K 252a

Pricing Availability   Qty
Cat.No. 1683 - K 252a | C27H21N3O5 | CAS No. 99533-80-9
Description: Protein kinase inhibitor
Alternative 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
Purity: ≥98% (HPLC)
Datasheet
Citations (6)
Reviews
Literature

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
Storage Desiccate at -20°C
Purity ≥98% (HPLC)
CAS Number 99533-80-9
PubChem ID 3035817
InChI Key KOZFSFOOLUUIGY-SOLYNIJKSA-N
Smiles [H][C@](C[C@]8(O)[C@@](OC)=O)(O[C@]78C)N5C3=C2N7C1=CC=CC=C1C2=C(CNC6=O)C6=C3C4=CC=CC=C45

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 11.69 25

Preparing Stock Solutions

The following data is based on the product molecular weight 467.48. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.25 mM 8.56 mL 42.78 mL 85.57 mL
1.25 mM 1.71 mL 8.56 mL 17.11 mL
2.5 mM 0.86 mL 4.28 mL 8.56 mL
12.5 mM 0.17 mL 0.86 mL 1.71 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

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

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

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


If you know of a relevant reference for K 252a, please let us know.

View Related Products by Product Action

View all Broad Spectrum Protein Kinase Inhibitor Inhibitors

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6 Citations for K 252a

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

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

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

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

Chen et al (2014) BDNF released during neuropathic pain potentiates NMDA receptors in primary afferent terminals. Eur J Neurosci 39 1439 PMID: 24611998


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