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Protein Kinase C (PKC)

Protein kinase C (PKC) inhibitors and activators act on a family of lipid-regulated serine/threonine kinases. Conventional PKC isoforms require calcium and diacylglycerol, novel isoforms need only diacylglycerol, and atypical isoforms respond to neither. Tumor-promoting phorbol esters mimic diacylglycerol and were shown in 1982 to activate PKC directly. 12-O-tetradecanoyl phorbol-13-acetate (TPA) is the standard activator of this kind, and ingenol mebutate also activates several isoforms. Staurosporine was first described as a PKC inhibitor but blocks a wide range of protein kinases. Enzastaurin is selective for PKCβ, while GO6983 and Ro 31-8220 mesylate inhibit multiple conventional and novel isoforms.

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  • 3-Methyl-L-tyrosine
    Cat. No.
    A46256
    CAS No.
    17028-03-4

    3-Methyl-L-tyrosine

    3-Methyl-L-tyrosine is a derivative of L-Tyrosine that features a methyl group at the third position of the aromatic ring. This compound acts as a substrate for the protein tyrosine kinase Csk, demonstrating a catalytic efficiency (kcat/Km) of 38% relative to L-Tyrosine, indicating its role in modulating the enzymatic processing of Gsk. Research applications of 3-Methyl-L-tyrosine include studying the molecular recognition mechanisms of Gsk's substrates, which is essential for the design of specific inhibitors targeting Gsk in various therapeutic areas.

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