NAPHTHOL AS-E PHOSPHATE

Biological Activity

Naphthol AS-E phosphate is a CREB inhibitor that disrupts CREB-dependent transcription (Ki=10 μM) and CREB:CBP interaction (Ki=50 μM). It also disrupts the binding of phosphorylated CREB (Ser-133) to KIX with a Ki of approximately 90 μM.

in vitro

Naphthol AS-E phosphate inhibited (or partially inhibited) the induction of cAMP-related genes by preventing CREB:CBP interaction. KG-501 inhibited neurite outgrowth, synaptogenesis and reduced MAP2+ neurons.

in vivo

Naphthol AS-E phosphate inhibited the expression of CREB, CCL2 and ERK phosphorylation, while significantly reducing cAMP levels. CREB may help to fight neuroinflammation through the cAMP/ERKadjustment pathway, thereby protecting nerves.It significantly promoted neurological function in a mouse model treated with azomethane oxide (AOM), reducing ERK phosphorylation levels and cAMP concentrations in the cortex.