Drug intelligence / Profile preview

GO-Y030

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

GO-Y030 is a **synthetic curcumin analog** developed to enhance the potency and bioavailability of curcumin. It demonstrates strong **antitumor activities** through several mechanisms, including: - Inhibiting **histone acetyltransferase p300 activity**, leading to suppression of histone acetylation at key gene regions (such as the Foxp3 promoter), thereby reducing regulatory T cell (Treg) generation and stability[1][3]. - Blocking **TGF-β-induced Foxp3 gene expression** and downstream regulatory T cell expansion in tumors, enhancing antitumor immunity[1]. - Inhibiting **STAT3 phosphorylation/activation**, which induces apoptosis and reduces viability of tumor cells, especially in cancer stem cells and cancer models such as melanoma and colorectal cancer[1][4]. - Inhibiting **tumor invasion and metastasis** by downregulating expression of TGF-β, matrix metalloproteinase 2 (MMP2), and VEGFα, blocking both glycolytic and metastatic pathways[2]. - GO-Y030 also ameliorates pathological cardiac hypertrophy and heart failure in preclinical models by inhibiting p300-HAT and subsequent histone acetylation[3]. GO-Y030 does not significantly affect normal vascular endothelial cells and shows greater potency at lower doses than curcumin in preclinical mouse studies[2][3].

Other names
curcumin analog GO-Y030
02

Targets

EP300 (Histone acetyltransferase p300)STAT3 (Signal Transducer and Activator of Transcription 3)HSP70 (Heat shock protein 70)

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