Neu Activators
Neu, also known as ErbB2 or HER2, is a transmembrane receptor tyrosine kinase that belongs to the epidermal growth factor receptor (EGFR) family. Unlike other EGFR family members, Neu lacks a ligand-binding domain and is activated through heterodimerization with other EGFR family members upon ligand binding. The primary function of Neu is to regulate cell growth, proliferation, differentiation, and survival through activation of downstream signaling pathways such as the PI3K-Akt and Ras-MAPK pathways. Dysregulation of Neu signaling is associated with various human cancers, particularly breast cancer, where Neu overexpression is a hallmark of aggressive tumors.
Activation of Neu occurs primarily through ligand-dependent heterodimerization with other EGFR family members, such as EGFR or HER3, upon binding of specific ligands such as heregulin or neuregulin. This heterodimerization leads to the transphosphorylation of tyrosine residues in the intracellular domain of Neu, triggering downstream signaling cascades that promote cell proliferation and survival. Additionally, Neu can also be activated in a ligand-independent manner through mechanisms such as receptor overexpression, gene amplification, or mutations in the receptor itself, leading to constitutive activation of downstream signaling pathways. These mechanisms contribute to oncogenic transformation and tumor progression in cancer cells expressing elevated levels of Neu. Understanding the mechanisms of Neu activation is crucial for the development of targeted therapies aimed at inhibiting aberrant Neu signaling in cancer.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Canertinib | 267243-28-7 | sc-207397 | 10 mg | $260.00 | 3 | |
Canertinib is a small-molecule tyrosine kinase inhibitor that indirectly activates Neu. By inhibiting the kinase activity, it may induce compensatory feedback loops leading to increased activation of Neu through altered signaling cascades. | ||||||
Lapatinib | 231277-92-2 | sc-353658 | 100 mg | $420.00 | 32 | |
Lapatinib is a dual tyrosine kinase inhibitor that targets both EGFR and Neu. Its inhibitory effects on these kinases can lead to feedback activation of downstream signaling pathways, indirectly enhancing Neu activation through altered cellular responses. | ||||||
Afatinib | 439081-18-2 | sc-364398 sc-364398A | 5 mg 10 mg | $114.00 $198.00 | 13 | |
Afatinib is a covalent inhibitor of the ERBB family, including Neu. While directly inhibiting the kinase activity, prolonged exposure to Afatinib may trigger compensatory mechanisms that enhance Neu activation, potentially through altered downstream signaling pathways. | ||||||
Neratinib | 698387-09-6 | sc-364549 sc-364549A sc-364549B sc-364549C sc-364549D | 5 mg 25 mg 100 mg 500 mg 1 g | $92.00 $214.00 $383.00 $755.00 $1250.00 | 4 | |
Neratinib is an irreversible pan-ERBB inhibitor that directly targets Neu. Its long-term exposure may induce compensatory mechanisms that lead to enhanced Neu activation, possibly through the modulation of downstream signaling cascades and cellular responses. | ||||||
4,4′-Diaminostilbene-2,2′-disulfonic Acid | 81-11-8 | sc-210166 | 100 g | $165.00 | ||
DAPH is an activator of Neu by promoting its phosphorylation and activation. The exact mechanism may involve direct interaction with Neu or modulation of signaling pathways leading to enhanced Neu activity, contributing to cellular processes associated with cancer. | ||||||
Heparin | 9005-49-6 | sc-507344 | 25 mg | $119.00 | 1 | |
Heparin activates Neu through indirect mechanisms. It may bind and sequester ligands or modulate the extracellular matrix, affecting Neu activation by promoting ligand-receptor interactions or influencing downstream signaling pathways associated with cell growth. | ||||||
AG 825 | 149092-50-2 | sc-202045 sc-202045A sc-202045B sc-202045C | 2 mg 5 mg 10 mg 100 mg | $47.00 $94.00 $183.00 $1769.00 | ||
AG825 is a selective Neu kinase inhibitor that, paradoxically, may induce compensatory feedback loops leading to enhanced Neu activation. Prolonged exposure to AG825 could result in altered downstream signaling cascades, contributing to increased Neu activity. | ||||||