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You are here:Home » Molecular Biology » MB-Protein Kinase Inhibitors » K252a

K252a

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Specifications

K252a is an alkaloid isolated from Nocardiopsis sp. soil fungi. This compound is a highly potent cell permeable CaM Kinase II inhibitor (IC50=1.8nM). At higher concentrations it also inhibits broad spectrum of protein kinases (18) . It is an excellent research tool of NGF receptors-trk-signal transduction due to its potent inhibition of trk-NGF receptor-tyrosine kinase activity.
Catalog #K0000-50A
K252a inhibits PKA, PKG, MLCK, PKC, CaMK, phosphorylase kinase, MAP kinase, the trk family of receptor tyrosine kinases and numerous other kinases by acting as a competitive inhibitor with respect to ATP. K252a binds to neuroblastoma membrane with high affinity (2.7nM). This compound is also observed to promote survival of primary neuronal cultures (75nM) and to induce neurite outgrowth in SH-SY5Y neuroblastoma cells, an event which is accompanied by enhanced phosphorylation of FAK.
Molecular Weight~4.7kD
Biological ActivityPKA: Ki =18nM
PKG: Ki =20nM
MLCK: Ki =17nM
PKC: Ki =25nM
CaMK: Ki =1.8nM
Phosphorylase Kinase: IC50 =1.7nM
Trk: IC50 =3nM
SolubilityDMSO (~1mg/ml); DMF (~1mg/ml)
Storage and StabilityLyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with DMSO or DMF. Aliquot to avoid repeated freezing and thawing. Store at -20°C. Reconstituted product is stable for 3 months at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
Molecular FormulaC27H21N3O5
Molecular Weight~4.7kD
Purity~98%
ConcentrationAs reported
FormSupplied as a lyophilized powder. Not sterile.
Important NoteThis product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.


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