14-3-3 Antagonist I, 2-5

A cell-permeable dipeptidyl-phosphoserine compound that effectively disrupts 14-3-3 interaction with its ligands (IC₅₀ = 2.6 µM against TMR-GG-RLSHpSSLPG binding to human 14-3-3ς), including Raf-1 and p53. Shown to induce caspase-3 activation and apoptotic cell death in human lung adenocarcinoma A549 cultures (100µM) in a time-dependent manner.

A cell-permeable dipeptidyl-phosphoserine compound that targets 14-3-3 phosphopeptide binding site and effectively competes against 14-3-3 ligands, including Raf-1 and p53, binding to 14-3-3 (IC₅₀ = 2.6 µM against TMR-GG-RLSHpSSLPG binding to human 14-3-3ς). Shown to induce caspase-3 activation and apoptotic cell death in human lung adenocarcinoma A549 cultures (live cell population after 12 h 100 µM drug treatment = 30% of control). Stability study using A549 cell lysates (100 µM drug in 1 µg/ml lysate) reveals a dephosphorylation t_1/2 of ~ 6 hrs and no detectable proteolytic degradation up to 12 hrs.

Packaged under inert gas

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Wu, H., et al. 2010. Angew. Chem. Int. Ed.49, 6528.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany