Drug intelligence / Profile preview

APTSTAT3-9R

Development stage
Preclinical
Modality
Peptides
Administration
Intratumoral, Intravenous
01

Overview

APTSTAT3-9R is a **STAT3-binding peptide inhibitor** designed to block activation of Signal Transducer and Activator of Transcription 3 (STAT3), a key regulator of proliferation, survival, metastasis, immune escape, and drug resistance in cancer cells[1][5][7]. It consists of a peptide discovered via phage display, fused to nine arginine residues to facilitate cell entry and binding via a GGGGS linker[5]. APTSTAT3-9R specifically inhibits STAT3 phosphorylation, DNA binding, and downstream gene expression without significant effect on STAT1, STAT5, or AKT pathways[1][5]. In vitro, it reduces STAT3-DNA-binding and induces apoptosis in cancer cell lines (A549, B16F1, HepG2) in a dose-dependent manner (IC50 10–20 μM)[1][5]. In vivo, intratumoral injection slows tumor growth in xenograft mouse models and resensitizes vemurafenib-resistant melanoma to therapy[1][3][5].

Brand names
APTSTAT3-9RAPTSTAT-3-9RAPTSTAT 3-9R
Other names
APT STAT3-9RSTAT3 Inhibitor XXSTAT-3 Inhibitor XXSTAT 3 Inhibitor XX
02

Targets

STAT3 (Signal Transducer and Activator of Transcription 3)

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