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).[2][3][4][5][6][7][8][9]
K252a is reported to promote myogenic differentiation in C2 mouse myoblasts[6] and has been shown to block the neuronal differentiation of rat pheochromocytoma PC12 cells by inhibition of trk tyrosine kinase activity.[10]
K252a has been reported in preclinical research as a potential treatment for psoriasis.[11]
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
- ^ K252a from Fermentek
- ^ 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.
- ^ Dubois Declercq, Sarah; Pouliot, Roxane (2013). “Promising New Treatments for Psoriasis”. The Scientific World Journal 980419. doi:10.1155/2013/980419. PMC 3713318. PMID 23935446.
Further reading
- Wood JL, Stoltz BM, Dietrich HJ (1995). “Total synthesis of (+)- and (−)-K252a”. J Am Chem Soc. 117 (41): 10413–4. Bibcode:1995JAChS.11710413W. doi:10.1021/ja00146a039.