Table 2 Application of STAT3 inhibitors in breast cancer treatment

BT474R/NCI-N87R

In vitro

S3I-201

NO

Inhibits STAT3 activation and sensitizes resistant cells to trastuzumab treatment

[186]

SUM159/BT549

In vitro/vivo

C188

NO

Inhibits STAT3 activation (SH2 domain) and ameliorates chemoresistant, like in combining with docetaxel

[187]

MDA-MB-231/ 435S

In vitro/vivo

Stattic

NO

Inhibits STAT3 activation, dimerization, and nuclear translocation

[188]

MDA-MB-468/ 435/MCF7

In vitro

STA-21

NO

Selectively inhibits STAT3 DNA binding capacity and dimerization (did not affect the STAT3 upstream regulators)

[189]

4T1/MCF-7/MDA-MB-231

In vitro/vivo

Nifuroxazide

NO

Inhibits STAT3 activation, MMP-2/9 expression; decreases MDSCs in lung cancer

[190]

MDA-MB-468/231

In vitro/vivo

Euc

NO

Inhibits STAT3 activation and nuclear translocation

[191]

MDA-MB-231/ 468

In vitro/vivo

DCV

NO

Selectively inhibits STAT3 activation, but does not affect the upstream JAK1/2 and silent STAT3

[192]

MCF-10A/7;

MDA-MB-231/468/T47D,

In vitro/vivo

ODZ10117

NO

Inhibits STAT3 activation (SH2 domain), regardless of other STAT family proteins and upstream regulators

[205]

Breast cancer sentinel lymphocyte

In vitro

AG490

NO

Inhibits the CpG-induced STAT3 activation; promotes DCs maturation and Th1 cells accumulation

[198]

4T1/MDA-MB-231/MCF-7

In vitro/vivo

Pectolinarigenin

NO

Inhibits STAT3 activation, MMP-2/9 expression; improves CD8⁺ T cells recruitation

[158]

4T1

in vitro/vivo

Alisertib

NO

Inhibits STAT3-mediated ROS generation in breast cancer; ameliorates MDSCs immunosuppressive function

[54]

TM40D-MB/TUBO

In vitro/vivo

Pyrimethamine (PYR)

NO

Blockes STAT3 activity; decreases the frequencies of Foxp3 + Tregs and promotes the CD8⁺ T cell

[30]

MDA-MB-231/468

In vitro/vivo

Niclosamide

YES

inhibits STAT3 and Bcl-2, and increases ROS generation in vitro and in vivo; it is identified as a radiosensitizer

[222]

SKBR3

In vitro/vivo

S3I-201

YES

Inhibits STAT3 activation (radiation-related) and increases radiation-induced cell death

[223]