Product Name: B-Raf (443-449) pS446+pS447
Product Number: PE-04AYT00
Size: | 200 µg | | Price: | 12.00 |
| 1 mg | | $US | 24.00 |
Peptide Name: B-Raf (443-449) pS446+pS447
Product Use: This phosphopeptide may be useful as a substrate for screening the phosphatase activity of protein phosphatases and for epitope mapping of phosphosite-specific antibodies. The peptide sequence is located just before the kinase catalytic domain. This is the major in vivo phosphorylation sites in B-Raf. S446 and S447 phosphorylation stimulate phosphotransferase activity and induces interaction with H-Ras-1.
Peptide Production Method: Solid-phase peptide synthesis
Peptide Origin: Homo sapiens
Peptide Sequence: RRD-pS-pS-DD
Peptide Modifications N Terminus: Free amino
Peptide Modifications C Terminus: Amide
Peptide Modifications Other: Phosphorylated
Peptide Molecular Mass Calculated: 1008.76 Da
Peptide Purity Percent after Synthesis and Purification: <70
Peptide Appearance: White powder
Peptide Form: Solid
Storage Conditions: -20°C
Scientific Background: B-Raf (RAFB1) is a protein-serine/threonine kinase of the TKL group and RAF family. It is a cytoplasmic kinase that participates in the RAS>RAF>MEK>ERK pathways, which is involved in the transduction of mitogenic signals from the cell membrane to the nucleus and promotion of cell division, differentiation, and cytokine secretion. Ras isoforms are inactive when bound to GDP, but when they are bound to GTP they become active and promote stimulation of B-Raf. Phosphorylation of S446 increases phosphotransferase activity and induces interaction with H-Ras-1. Phosphorylation of S579, T599, and S602 increases B-Raf phosphotransferase activity. Phosphorylation of S729 increases phosphotransferase activity and induces interaction with 14-3-3 beta. Phosphorylation of S365, S429, and T440 inhibits phosphotransferase activity. Phosphorylation of T753 inhibits interaction with Raf1. B-Raf is expressed in most tissues with high expression in neuronal tissue. The transcription of several genes have been found to be increased by this pathway, including cyclins D1, D2 and D3, VEGF, c-myc, b3-integrin and mdm2. B-Raf is a known oncoprotein (OP). Cancer-related mutations in human tumours point to a gain of function of the protein kinase. Gain-of-function mutations in B-Raf are estimated to be present in ~15-19% of all human cancers, and 66% of malignant melanomas have been identified with a B-Raf somatic missense mutation. A single point mutation (V600E), located in the kinase catalytic domain in the activation loop between Subdomains VII and VIII. It has been reported to account for ~80% of the B-Raf mutations in human cancers. Mutated B-Raf proteins display constitutive elevated levels of phosphotransferase activity, resulting in the aberrant promotion of cell division, differentiation, and cytokine secretion.
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