K252a

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K252a is an alkaloid isolated from Nocardiopisis sp. soil fungi. This ATP analog is a highly potent cell permeable inhibitor of CaM kinase and phosphorylase kinase (IC50 = 1.8 and 1.7 nmol/L, respectively). At higher concentrations it is also an efficient inhibitor of serine/threonine protein kinases (IC50 of 10 to 30 nmol/L).(1-8)

K252a is reported to promote myogenic differentiation in C2 mouse myoblasts 9 and has been shown to block the neuronal differentiation of rat pheochromocytoma PC12 cells by inhibition of trk tyrosine kinase activity.(10) Paradoxically K252a exerts neurotrophic effects on primary sensory neurons, neuroblastoma cells, PC12 cells, and central neurons.(11-13)

K252a inhibits tyrosine phosphorylation of Trk A induced by NGF. PC12 cells were incubated in the presence or absence of 10 ng/ml NGF with or without various concentrations of K252a.

Physical and chemical data

UV spectrum: 205, 250, 289, 334, 367 nm

Solubility: DMSO, dichloromethane, methanol

CAS number : 97161-97-2

Molecular weight: 467.5

Molecular formula: C27H21N3O5

References

1. Ruegg, U.T. et al. (1989) Tips 10, 218.

2. Eliot, L.H. et al. (1990) B.B.R.C. 171, 148.

3. Simpson, D.l. et al. (1991) J. Neurosci. Res, 28, 148.

4. Chin, L.S. et al. (1999) Cancer Invest. 17, 391.

5. Tapley, P. et al. (1992) Oncogene 7, 371.

6. Hashimoto, S. (1998) J. Cell Biol. 107, 1531.

7. Kase, H. et al. (1987) B.B.R.C. 142, 436.

8. Hirayama E. et al. (2001) B.B.R.C. 285, 1237.

9. Tapley, P. et al. (1992) Oncogene 7, 371.

10.Borasio, G.D. Neurosci. Lett. (1990) 108, 207.

11.Hashimoto, S. et al. (1989) Exp. Cell Res. 184, 351.

12.Tischler, A.S. et al. (1991) J. Biol. Chem. 266, 1141.

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