Drug intelligence / Profile preview

naphthol AS-E phosphate

Development stage
Preclinical
Modality
Small Molecules
01

Overview

Naphthol AS-E phosphate is a synthetic small molecule, chemically known as N-(4-chlorophenyl)-3-(phosphonooxy)naphthalene-2-carboxamide. It is primarily used as a histochemical substrate for alkaline phosphatases and has been studied as an aldolase inhibitor. In cancer research, it acts as an anticancer compound by directly targeting the KIX domain of CBP (CREB-binding protein), thereby disrupting the CREB-CBP complex, inhibiting CREB-target gene induction, and suppressing IL‑1β-mediated angiogenic activity in cancer cell lines. Additionally, it inhibits the activity of transcription factor Myb by blocking its interaction with the KIX domain of coactivator p300 in human leukemia cells. This interference leads to suppression of Myb target genes and induces myeloid differentiation and apoptosis[3].

Other names
N-(4-chlorophenyl)-3-(phosphonooxy)naphthalene-2-carboxamide({3-[(4-chlorophenyl)carbamoyl]naphthalen-2-yl}oxy)phosphonic acid3-(phosphonooxy)naphthalene-2-carboxamide
02

Targets

CREBBP (CREB-binding protein)EP300 (Histone acetyltransferase p300)

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