K 252a

Cat. No. 1683 7 Citations Submit a Review Datasheet / COA / SDS

Pricing	Availability		Qty

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 (7)

Reviews

Biological Activity Technical Data Solubility Calculators Datasheets References

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 Data 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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Product Datasheets for K 252a

Certificate of Analysis / Product Datasheet

Safety Datasheet

References for K 252a

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.

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