KG-501 (Naphthol AS-E phosphate)

Naphthol AS-E phosphate is an inhibitor of the protein-protein interaction between CREB and the KIX domain of CREB-binding protein (CBP; K_i = 50 ?M).¹ It also inhibits the binding of the transcription factor Myb to the KIX domains of p300 and CBP (IC₅₀s = 30 and 43 ?M, respectively).² Naphthol AS-E phosphate inhibits CREB-dependent transcription in HEK293T cells (K_i = 10 ?M).¹ It also decreases the expression of Myb target genes and induces differentiation in HL-60, U937, and NB4 myeloid leukemia cells when used at a concentration of 5 ?M.² Naphthol AS-E phosphate inhibits proliferation of NCI-H1734 lung adenocarcinoma cells (IC₅₀ = 6.89 ?M).³

1.Best, J., Amezcua, C.A., Mayr, B., et al.Identification of small-molecule antagonists that inhibit an activator: Coactivator interactionProc. Natl. Acad. Sci. USA101(51)17622-17627(2004) 2.Uttarkar, S., Dukare, S., Bopp, B., et al.Naphthol AS-E phosphate inhibits the activity of the transcription factor Myb by blocking the interaction with the KIX domain of the coactivator p300Mol. Cancer Ther.14(6)1276-1285(2015) 3.Lee, J.W., Park, H.S., Park, S.-A., et al.A novel small-molecule inhibitor targeting CREB-CBP complex possesses anti-cancer effects along with cell cycle regulation, autophagy suppression and endoplasmic reticulum stressPLoS One10(4)e0122628(2015)