Product Name: PKCA/BSubtide
Product Number: PE-01BIR95
Size: 200 µg      Price:45.00
1 mg      $US91.00
Peptide Name: PKCA/BSubtide

Product Use: For assaying the phosphotransferase activity of Protein-serine kinase C alpha (UniProt ID P17252).

Peptide Production Method: Solid-phase peptide synthesis

Peptide Sequence: KRFRRKSFRRKG

Peptide Modifications N Terminus: Free amino

Peptide Modifications C Terminus: βAla-Cys

Peptide Molecular Mass Calculated: 1795.19 Da

Peptide Purity Percent after Synthesis and Purification: >50

Peptide Appearance: White powder

Peptide Form: Solid

Storage Conditions: -20°C

Peptide Recommended Enzyme: PKCA/B

Scientific Background: PKCa (PRKCA, PKC-alpha) is a protein-serine/threonine kinase in the classical protein kinase C family. This kinase is moderate to highly expressed in most tested human tissues. It is calcium activated, and dependent on acidic phospholipids (e.g. phosphatidylserine) and diacylglycerol for full phosphotransferase activity. Fatty acids can also activate PKCa. Phosphorylation of T494, T495 and T497 increases kinase activity. Phosphorylation of S657 increases phosphotransferase activity, protects against dephosphorylation of the T497 site and degradation of PKC-alpha. Phosphorylation of T638 is not essential for catalytic activity, but it protects against dephosphorylation of the T497 site. PKCa has been identified as a fundamental regulator of cardiac contractility and Ca(2+) handling in myocytes. PKCa has been linked with the development of colon, pituitary and thyroid cancers as well as glioblastoma multiforme (GM). PKCa has been considered as an oncoprotein (OP), since during tumourigenesis, as it is strongly activated by many different tumour promoting compounds, such as phorbol esters and teleocidins. While these compounds promote binding of PKC isoforms to the plasma membrane of cells, which stimulates their phosphotransferase activity, these agents also induce rapid down-regulation of PKC isoforms. Consequently, PKCa may be actually be a tumour suppressor protein. PKCa is highly expressed in several cancers, including malignant breast cancers and gliomas. Increased expression of PKCa has been observed in adenomatous pituitaries, with highest expression in invasive pituitary tumours. A point mutation was also identified in 4 invasive pituitary tumours. Furthermore, PKCa appears to stimulate cell proliferation, because many of its direct targets, such as Raf1, Bcl2, and CSPG4, participate in growth factor signalling pathways and PKC activators induce the downstream activation of ERK1/2 (MAPK3/1) and RAP1-GAP.