L803

Product Name:L803

CAS No:348089-28-1

Purity:95%

Molar Mass:1198.23

Chemical Formula:C50H80N13O19P

Storage:Store at -20 degrees Celsius

Sequence:KEAPPAPPQSP

Target:substrate-competitive inhibitor of GSK-3β

Application:L803 is a synthetic peptide that acts as an inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) signaling pathway. IGF-1R plays a critical role in cell growth, survival, and metabolism, making it a key target in research focused on cancer, metabolic disorders, and aging. L803 specifically binds to IGF-1R, blocking its activation and subsequent downstream signaling. By inhibiting IGF-1R, L803 disrupts processes such as cell proliferation and resistance to apoptosis, making it a valuable tool for studying the role of IGF-1R in disease progression and for exploring potential therapeutic strategies targeting this pathway in cancer and other IGF-1R-related conditions.

Current Research:

L803 (CAS: 348089-28-1) is a synthetic phosphopeptide derived from the glycogen synthase kinase-3 (GSK-3) recognition motif. It functions as a substrate-competitive inhibitor of GSK-3β, with an inhibitory concentration (IC₅₀) of 150 μM. Notably, L803 exhibits minimal inhibition of other kinases, including Cdc2, MAPK, PKA, CK2, PKCδ, and PKB, even at concentrations up to 200 μM, underscoring its selectivity for GSK-3β.

Chemical Properties

Modifications: Phosphorylation at Serine-10

Mechanism of Action

L803 competitively binds to the substrate recognition site of GSK-3β, thereby inhibiting its kinase activity. This inhibition can modulate various cellular processes regulated by GSK-3β, including glycogen metabolism, gene expression, and cell differentiation.

Research Applications

Due to its specificity, L803 is utilized in research to:

Investigate the role of GSK-3β in cellular signaling pathways.

Explore therapeutic strategies for diseases where GSK-3β is implicated, such as diabetes, neurodegenerative disorders, and certain cancers.

Handling and Storage

For optimal stability, L803 should be stored desiccated at -20°C. It is soluble in water up to 1 mg/mL, facilitating its use in various experimental protocols.

Conclusion

L803 serves as a valuable tool for probing the functions of GSK-3β in biological systems and holds potential for the development of therapeutic interventions targeting GSK-3β-related pathways.

Reference:

Kaidanovich-Beilin, O., & Eldar-Finkelman, H. (2006). Long-term treatment with novel glycogen synthase kinase-3 inhibitor improves glucose homeostasis in ob/ob mice: molecular characterization in liver and muscle. Journal of Pharmacology and Experimental Therapeutics, 316(1), 17-24.