K252a
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| K252a | |
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-K252a.svg/200px-(+)-K252a.svg.png) |
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-K252a_1R0P.png/200px-(+)-K252a_1R0P.png) |
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| Identifiers | |
| CAS number | |
| PubChem | |
| Properties | |
| Molecular formula | C27H21N3O5 |
| Molar mass | 467.47 g mol-1 |
| Except where noted otherwise, data are given for materials in their standard state (at 25 °C, 100 kPa) Infobox disclaimer and references |
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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][2][3][4][5][6][7][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][12]
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.
[edit] Physical and chemical data[13]
UV spectrum: 205, 250, 289, 334, 367 nm
Solubility: DMSO, dichloromethane, methanol
CAS number : 97161-97-2
Molecular weight: 467.5
Molecular formula: C27H21N3O5
[edit] References
- ^ 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.
- ^ 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.
- ^ Tapley, P. et al. (1992) Oncogene 7, 371.
- ^ Borasio, G.D. Neurosci. Lett. (1990) 108, 207.
- ^ Hashimoto, S. et al. (1989) Exp. Cell Res. 184, 351.
- ^ Tischler, A.S. et al. (1991) J. Biol. Chem. 266, 1141.
- ^ *A vendor product page about K252A: K252a from Fermentek.
[edit] Further reading
- Wood JL, Stoltz BM, Dietrich H-J (1995). "Total synthesis of (+)- and (−)-K252a". J Am Chem Soc 117 (41): 10413–4. doi:.
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