5-hydroxy-2-(1'-hydroxyethyl)naphtho[2,3-b]furan-4,9-dione

STAT3-IN-14 (Compound 1) is a STAT3 inhibitor and has STAT3 phosphorylation inhibitory activity. STAT3-IN-14 (Compound 1) can directly bind to the hinge region of STAT3[1].

Signaling Pathways >> Stem Cell/Wnt >> STAT

Research Areas >> Cancer

Signaling Pathways >> JAK/STAT Signaling >> STAT

IC50: 0.42 μM (MDA-MB-231); 0.50 μM (MCF7); 0.13 μM (A549) [1]

STAT3-IN-14 (Compound 1) shows inhibitory activity against phosphor-STAT3. STAT3-IN-14 (Compound 1) reduces the phosphorylation inhibitory activity against MDA-MB-231 cells (JAK/STAT pathway constitutively active) in does dependent manner, but no inhibitory activities against JAK kinases. STAT3-IN-14 (Compound 1) has growth inhibitory activity with with IC50 values of 0.42 μM, 0.50 μM and 0.13 μM in MDA-MB-231, MCF7 and A549cells, respectively[1]. Western Blot Analysis[1] Cell Line: MCF7 cells; MDA-MB-231 cells Concentration: 1 or 10 μM; 0.5, 1, 2, 4 μM Incubation Time: 1 h; 2 h Result: Completely inhibited STAT3 phosphorylation at 10 μM, and partial inhibition at 1 μM. Reduced the phosphorylation of STAT3 in does dependent manner. Cell Proliferation Assay[1] Cell Line: MDA-MB-231, MCF7 and A549 cells Concentration: 0-30 μM Incubation Time: 72 h Result: Showed moderate to strong growth inhibitory activity among the three cancer cell lines.

[1]. Teruyuki Tahara, et al. STAT3 inhibitory activity of naphthoquinones isolated from Tabebuia avellanedae. Bioorg Med Chem. 2020 Mar 15;28(6):115347.