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.
1. Kase, H., et al. 1986. J. Antibiot. 39: 1059-1065. PMID: 3759657
2. Kase, H., et al. 1987. Biochem. Biophys. Res. Commun. 142: 436-440. PMID: 3028414
3. Hashimoto, Y., et al. 1991. Biochem. Biophys. Res. Commun. 181: 423-429. PMID: 1659814
4. Tapley, P., et al. 1992. Oncogene. 7: 371-381. PMID: 1312698
5. Cheng, B., et al. 1994. J. Neurochem. 62: 1319-1329. PMID: 7510777
6. Glicksman, M.A., et al. 1995. J. Neurochem. 64: 1502-1512. PMID: 7891076
See how others have used K-252a. Click on the entry to view the PubMed entry .
PMID: # 28495385 Moosavi, F. et al. 2017. Bioorg. Med. Chem. 25: 3235-3246.
PMID: # 18955270 Hattori, N. et al. 2010. Evid Based Complement Alternat Med. 7: 63-8.
PMID: # 17266195 Hudkins, RL. et al. 2007. J. Med. Chem. 50: 433-441.
PMID: # 17396254 Kim, SY. et al. 2007. Appl. Microbiol. Biotechnol. 75: 1119-1126.
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