K-252a is a metabolite originally isolated from the culture broth of Nocardiopsis sp.. Experiments have shown that at high concentrations this compound is an ATP-competitive inhibitor of cyclic nucleotide-dependent protein kinases. More specifically, K-252a has been found to be a potent inhibitor of PKA, PKC (protein kinase C) activity (IC50 = 32.9 nM), Ser/Thr kinase, CaMKII, MYLK, and Met. K-252a is able to bind neuroblastoma, promoting survival of primary neuronal cultures and induction of neurite outgrowth in SH-SY5Y neuroblastoma cells, along with phosphorylation of tyrosine kinase. Additionally, K-252a also has demonstrated the ability to block neuronal differentiation of rat pheochromocytoma pC12 cells induced by nerve growth factor (NGF) at high concentrations. At very low concentrations (10fM-10nM), K-252a has been noted to prolong the survival of septal, hippocampal, and cortical neurons deprived of glucose. K-252a is an inhibitor of Cdc2, Cdc25, cGKI, PHK, Trk A and PKN.
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See how others have used K-252a. Click on the entry to view the PubMed entry .
PMID: # 30763105 2019. Mol. Pharm. 16: 1423-1432.
PMID: # 28495385 Moosavi, F. et al. 2017. Bioorg. Med. Chem. 25: 3235-3246.
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