Recombinant human ERBB2 (HER2, HER-2), protein kinase domain, 10 µg

Background: The human epidermal growth factor receptor HER2/erbB2 is part of the erbB family of receptor tyrosine kinases, including also EGFR/erbB1, HER3/erbB3 and HER4/erbB4. Activation of ErbB receptors is initiated by ligand binding to their extracellular domain, leading to the formation of homo- and heterodimeric ErbB receptor complexes. Whereas ErbB1 and ErbB4 can form ligand induced active homo- and heterodimers there is no known ligand for ErBb2. Thus, Erbb2 is only activated upon recruitment and heterodimerization with other ErbB members (mainly ErbB3). Once activated, the signal is transmitted through different pathways, specifically the MAPK pathway, activation of PLCγ, PI3K stimulation of AKT signaling, and finally by the JAK/STAT pathway. HER2/ErbB2 is amplified and/or overexpressed in different human tumors, especially in breast but also in ovary, lung and stomach. Thus, HER2/ErbB2 is a major therapeutic target in cancer theraphy.

Protein: human ERBB2 kinase domain (amino acids Q679-V1255 (as in NCBI/Protein entry NP_004439.2), contains N-terminal GST fusion tags with thrombin cleavage sites
Theoretical MW (ERBB2): 93.9 kDa (fusion protein)
Expression system: Sf9 cells
Purification: One-step affinity purification using glutathione agarose
Storage buffer:  50 mM HEPES, pH 7.5, 100 mM NaCl, 5 mM DTT, 15 mM reduced glutathione, 20% glycerol
Protein concentration: 0.224 mg/ml (Bradford method using BSA as standard protein)
Method for determination of Km value & specific activity: Filter binding assay MAFC membrane
Specific activity: 36,000 pmol/mg min

Entrez Gene ID: 2064
UniProtKB:  P04626

Ordering information: shipped on dry ice

Product specific literature:

Landgraf R.(2007) " HER2 therapy. HER2 (ERBB2): functional diversity from structurally conserved building blocks." Breast Cancer Res, 9(1):202

Badache A, Gonïzalves A. Tetsuya Mitsudomi, MD.(2008) "The ErbB2 signaling network as a target for breast cancer therapy." J Mammary Gland Biol Neoplasia. 11(1):13-25.

Hynes NE, Horsch K, Olayioye MA, Badache A.(2008) "The ErbB receptor tyrosine family as signal integrators". Endocr Relat Cancer. 8(3):151-9.

Product Citations:

Wilson JN, Liu W, Brown AS, Landgraf R. (2015) "Binding-induced, turn-on fluorescence of the EGFR/ERBB kinase inhibitor, lapatinib." Org Biomol Chem.7;13(17):5006-11.