K252a
| K252a | |
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(9S-(9α,10β,12α))-2,3,9,10,11,12-hexahydro-10-hydroxy-10-(methoxycarbonyl)-9-methyl-9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocin-1-one |
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| Identifiers | |
| CAS number | 99533-80-9  |
| PubChem | 3035817 |
| ChemSpider | 2299962 |
| UNII | IV7H45AM5B  |
| ChEMBL | CHEMBL281948 |
| IUPHAR ligand | 336 |
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| Properties[1] | |
| Molecular formula | C27H21N3O5 |
| Molar mass | 467.47 g mol−1 |
| Solubility in other solvents | Soluble in DMSO, dichloromethane, and methanol |
 (verify) (what is:  / ?)Except where noted otherwise, data are given for materials in their standard state (at 25 °C, 100 kPa) |
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| Infobox references | |
K252a is an alkaloid isolated from Nocardiopisis sp. soil fungi. 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.[citation needed]
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] 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.
[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:10.1021/ja00146a039.
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