PKC

The protein kinase C (PKC; EC 2.7.11.13) family represents a large group of phospholipid dependent enzymes catalyzing the covalent transfer of phosphate from ATP to serine and threonine residues of proteins, mediating signal transduction for cell proliferation, differentiation, apoptosis and angiogenesis. The PKC family consists of at least twelve members, divided into three subgroups: the classical PKCs (cPKCs: PKCα, PKCβI, PKCβII, and  PKCγ), which are Ca2+ dependent and activated by both phosphotidylserine (PS) and diacylgylcerol (DAG); novel PKCs (nPKCs: PKCδ, PKCε, PKCη, and PKCθ), which are Ca2+ independent and regulated by DAG and PS; and atypical PKCs (aPKCs: PKCζ, PKCλ), which are Ca2+ independent and do not require DAG for activation, although PS can regulate their activity[1]. Many of these kinases show overlapping substrate specificities in vitro. Consistent with their different biological functions, PKC isoforms differ in their structure, tissue distribution, subcellular localization, mode of activation and substrate specificity. Early observations that PKC isozymes are activated by tumor-promoting phorbol esters suggested a key role for PKC in tumor promotion and progression leading to PKC being considered as a target for cancer therapy[2]

AGC kinases listed: PKAPKCPKD


[1] Protein kinase C pharmacology: refining the toolbox. A.X. Wu‑Zhang, A.C.Newton. Biochem. J. 2013, 452, 195-209.
[2] Targeting the protein kinase C family: are we there yet? H.J. Mackay, C.J. Twelves. Nat. Rev. Cancer 2007, 7, 554-562.

5 Item(s)

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Axon ID Name Description From price
2717 Apigenin Selective inhibitor of Casein kinase 2 (CK2) €70.00
3936 Bisindolylmaleimide I Potent and selective PKC inhibitor €120.00
3939 Bisindolylmaleimide IV Potent PKC inhibitor €120.00
3851 LXS-196 Potent and selective protein kinase C inhibitor Inquire
3986 N-Desmethyltamoxifen hydrochloride Metabolite of Tamoxifen (Axon 3252); PKC inhibitor €180.00

5 Item(s)

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