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Phorbol 12-myristate 13-acetate
Chemical Name:(1aR,1bS,4aR,7aS,7bS,8R,9R,9aS)-9a-(Acetyloxy)-1a,1b,4,
4a,5,7a,7b,8,9,9a-decahydro-4a,7b-dihydroxy-3-(hydroxym
ethyl)-1,1,6,8-tetramethyl-5-oxo-1H-cyclopropa[3,4]benz
[1,2-e]azulen-9-yl tetradecanoate
Biological Activity:
Extensively used phorbol ester activator of protein kinase C;
tumour promoter. Binds to PKC with a Ki value of 2.6 nM as measured
by displacement of [3H]phorbol 12,13-dibutyrate binding in rat
cortex synaptosomal membranes.
Merck
Index 12 7487. Castagnaet al (1982) Direct
activation of calcium-activated, phospholipid-dependent protein kinase by
tumor-promoting phorbol esters. J.Biol.Chem. 257 7847. Hockbergeret al (1989) A diacylglycerol analogue reduces neuronal calcium currents
independently of protein kinase C activation. Nature 338 340. Murphyet al (1999) Structural determinants of phorbol ester binding in
synaptosomes: pharmacokinetics and pharmacodynamics. Eur.J.Pharmacol. 381
77.