Product Name: InsR (1183-1195 ) pY1189
Product Number: PE-04AAJ90
Size: 1 mg      Price:52.00
5 mg      $US104.00
20 mg      244.00
Peptide Name: InsR (1183-1195 ) pY1189

Product Use: This phosphopeptide may be useful as a substrate for screening the phosphatase activity of protein phosphatases. The peptide sequence is located in the kinase activation loop between catalytic subdomains VII and VIII. Stimulates phosphotransferase activity, receptor internalization and induces interaction with SOCS1, IRS2 and PTP1B.

Peptide Production Method: Solid-phase peptide synthesis

Peptide Origin: Homo sapiens

Peptide Sequence: DIYETD-pY-YRKGGK

Peptide Modifications N Terminus: Free amino

Peptide Modifications C Terminus: Amide

Peptide Modifications Other: Phosphorylated

Peptide Molecular Mass Calculated: 1987.7 Da

Peptide Purity Percent after Synthesis and Purification: >90

Peptide Appearance: White powder

Peptide Form: Solid

Storage Conditions: -20°C

Scientific Background: InsR (IR) is a protein-tyrosine kinase of the TK group and InsR family. It binds and mediates the effects of insulin. Binding of insulin to the receptor results in the downstream phosphorylation of several intracellular signalling components, including insulin receptor substrates (IRS1, 2, 3, 4), Shc, GAB1, CBL, and other intracellular signalling intermediates. Phosphorylated IRS1 recruits and activates the GRB2/SOS complex, which in turn leads to the activation of the Ras/Raf/MAP2K/MAPK signalling pathway. This pathway is mainly involved in the regulation of cell growth, survival, and cellular differentiation resulting from insulin signalling. Insulin binds to InsR to trigger autophosphorylation at many sites, including Y999, S1001, Y1185, Y1189, Y1190, S1332, S1333, Y1355, Y1361 and T1375, which increases its phosphotransferase activity. Protein interactions are induced with phosphorylation of Y999 (with SOCS3) and Y1185, Y1189 and Y1190 (with IRS2 and PTP1B). Phosphorylation of Y992 and Y1011 inhibits the phosphotransferase activity of InsR. Binding of insulin to the InsR stimulates glucose uptake. Insulin receptor signalling helps to maintain fuel homeostasis and prevent diabetes. InsR signalling also increases the regeneration of adult beta-cells and the central control of nutrient homeostasis. InsR has also been linked with the development of insulin resistance, familial hyperinsulinemic hypoglycemia Type 5 (HHF5), and gastric adenocarcinomas. InsR appears to be an oncoprotein (OP). Over activation of the insulin receptor signalling pathway has been linked to the development of several cancer types, including breast cancer. In addition, elevated InsR expression in breast cancer is correlated with poor patient survival.