K252a
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| Solubility in other solvents | Soluble in DMSO, dichloromethane, and methanol |
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K252a is an alkaloid isolated from Nocardiopsis bacteria. This staurosporine 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][2][3][4][5][6][7][8]
K252a is reported to promote myogenic differentiation in C2 mouse myoblasts[5] and has been shown to block the neuronal differentiation of rat pheochromocytoma PC12 cells by inhibition of trk tyrosine kinase activity.[9]
K252a has been reported in preclinical research as a potential treatment for psoriasis.[10]
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.
See also
References
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- ↑ Ruegg, U.T. et al. (1989) Tips 10, 218.
- ↑ Eliot, L.H. et al. (1990) B.B.R.C. 171, 148.
- ↑ Simpson, D.l. et al. (1991) J. Neurosci. Res, 28, 148.
- ↑ Chin, L.S. et al. (1999) Cancer Invest. 17, 391.
- ↑ a b Tapley, P. et al. (1992) Oncogene 7, 371.
- ↑ Hashimoto, S. (1998) J. Cell Biol. 107, 1531.
- ↑ Kase, H. et al. (1987) B.B.R.C. 142, 436.
- ↑ Hirayama E. et al. (2001) B.B.R.C. 285, 1237.
- ↑ Borasio, G.D. Neurosci. Lett. (1990) 108, 207.
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Further reading
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