K 252a

Name: K 252a
Brand: Tocris Bioscience
SKU: 1683

Tocris Bioscience, part of Bio-Techne | Catalog # 1683

Citations (80)

COA / SDS

Protein kinase inhibitor

Key Product Details

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)
Molecular Weight:	467.48

View Full Technical Details for K 252a

Technical Data
Citations

Biological Activity for K 252a

K 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 (K_i = 20 nM) and receptor tyrosine kinases. Inhibits the oncogenic properties of MET; prevents autophosphorylation and activation of downstream effectors (MAPK, Akt).

Technical Data for K 252a

M. Wt	467.48
Formula	C₂₇H₂₁N₃O₅
Storage	Store 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 for K 252a

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

Preparing Stock Solutions for K 252a

The following data is based on the product molecular weight 467.48.

Batch specific molecular weights may vary from batch to batch due to the degree 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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References for K 252a

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

Ruegg and Burgess Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases. TiPS 1989 PMID: 2672462
Knusel and Hefti K-252 compounds: modulators of neurotrophin signal transduction. J.Neurochem. 1992 PMID: 1431889
Morotti K252a inhibits the oncogenic properties of Met, the HGF receptor. Oncogene 2002 PMID: 12118367
Kase K-252a, a potent inhibitor of protein kinase C from microbial origin. J.Antibiot. 1986 PMID: 3759657