WR-S-462 is a STAT3 inhibitor. WR-S-462 effectively suppresses STAT3 phosphorylation and biological functions in vitro. WR-S-462 inhibits MDA-MB-231 cells with an IC50 of 0.03 μM. WR-S-462 displays a strong binding affinity towards the STAT3 protein with a Kd of 58 nM. WR-S-462 inhibits the nuclear translocation of p-STAT3, selectively inhibits the expression of p-STAT3Tyr705 and downstream target genes regulated by STAT3 in MDA-MB-231 cells such as Cyclin D1, Bcl-2, and Bcl-xl. WR-S-462 inhibits TNBC (triple-negative breast cancer) growth and metastasis.

NW16 is an orally active inhibitor for STAT3 with Kd of 11.0 μM. NW16 arrests the cell cycle at S phase, induces apoptosis in HCT116, and inhibits the proliferation of cancer cell HCT116, A549, and B16 with IC50s of 0.28, 1.22, and 9.86 μM, respectively. NW16 induces the production of ROS, inhibits the PI3K/AKT signaling pathway, and thus exhibits antitumor efficacy in mouse model.

STAT3-SH2 domain inhibitor 1 is a potent Src Homology 2 (SH2) Domain of STAT3 (STAT3-SH2 domain) inhibitor with a Kd value of 1.57 μM. STAT3-SH2 domain inhibitor 1 inhibits STAT3 signaling transduction and transcriptional activation. STAT3-SH2 domain inhibitor 1 induces apoptosis in gastric cancer cells. STAT3-SH2 domain inhibitor 1 can be used in research of cancer.

Piperlongumine induces cell death and increases the level of reactive oxygen species (ROS) in cancer cells with both wild-type and normal p53.

CMD178 is a lead peptide that consistently reduced the expression of Foxp3 and STAT5 induced by IL-2/s IL-2Rα signaling. CMD178 also is an inhibitor of STAT5 and inhibit Treg cell development.

WZ-2-033 is a potent, selective STAT3 inhibitor, binds to the SH2 domain of the STAT3 protein with KD of 7.4 uM, disrupts STAT3 dimerization and significantly inhibits STAT3 signaling.

WB737 is a potent and selective STAT3 inhibitor, directly binds to the STAT3 Src homology 2 (SH2) domain with KD value of 1.34 nM.

WB436B is a potent and highly selective small molecule inhibitor of STAT3, specifically targets the STAT3-SH2 domain with KD value of 94.3 nM.

W2014-S is a small molecule STAT3 inhibitor with binding Kd of 3.64 uM, disrupts STAT3 dimerization and selectively inhibits STAT3 signaling.

W1131 is a potent and selective STAT3 inhibitor with Kd of 7.55 uM in surface plasmon resonance (SPR) assays, inhibits STAT3 Tyr705 phosphorylation, triggers ferroptosis and possesses potent anti-tumor effects both in vitro and in vivo.

TR120 (TR-120) is a potent small molecule STAT5 inhibitor, exhibits antiproliferative in K562 cells with IC50 of 0.12 uM, decreases STAT5 expression in imatinib-sensitive and imatinib-resistant BCR-ABL-expressing leukemia cells.

SF-1-088 is a small molecule STAT5-SH2 domain inhibitor with Ki of 8.3 uM (Stat5b), shows no affinity for Stat1 and Stat3 (Ki>25 uM).

ODZ10117 is a small molecule inhibitor of STAT3, effectively inhibits the level of tyrosine phosphorylated STAT3 in various cancer cell lines.

MNS1-MV is a novel pyrazole-based small molecular inhibitor of STAT3 pathway, potently inhibit IL-6-induced STAT3 phosphorylation at 10 μM in dBT114 cells.

MNS1-Leu is a novel pyrazole-based small molecular inhibitor of STAT3 pathway, potently inhibit IL-6-induced STAT3 phosphorylation at 10 μM in dBT114 cells.

MC0704 (MC-0704) is a novel synthetic STAT3 pathway inhibitor, exhibits potential antitumor activity in vitro and in vivo models in docetaxel-resistant TNBC cells.

LLL12B is a selective STAT3 inhibitor that suppresses Th17 development, specifically inhibits STAT3 and suppresses Th17 differentiation and expansion.

K1836 is a small molecule Stattic analog inhibitor of STAT3 signalling.

DR-1-55 (DR-155) is a selective STAT3 inhibitor that covalently modifies a cysteine in the SH2 domain of STAT3.

Colivelin is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin has the potential for the treatment of alzheimer's disease and ischemic brain injury

FLLK31 is a potent and selective inhibitor of the STAT3 signaling pathway.

Stat5 Inhibitor is a cell permeable nonpetidic nicotinoyl hydrazone which suppresses Stat5 via binding to the SH2 domain.

Napabucasin (BBI608) is an orally-administered small molecule which can block cancer stem cell (CSC) self-renewal and induces cell death in CSCs as well as non-stem cancer cells.

FLLL32, a novel curcumin analogue, is a potent STAT3 inhibitor.

C188-9 is a potent inhibitor of STAT3 that binds to STAT3 with high affinity (KD=4.7±0.4 nM). C188-9 is well tolerated in mice, shows good oral bioavailability, and is concentrated in tumors.

AS1517499 is a potent STAT6 inhibitor with IC50 of 21 nM.

inS3-54A18 is a potent inhibitor of STAT3 with anti-cancer properties.

GYY4137 is a novel, water-soluble hydrogen sulfide (H2S)–releasing molecule with vasodilator and antihypertensive activity. GYY4137 shows potent anti-hepatocellular carcinoma activity through blocking the STAT3 pathway. GYY4137 also shows anti-inflammatory activity.

STX-0119 is a selective, orally active STAT3 dimerization inhibitor. STX-0119 inhibits STAT3 transcription with an IC50 of 74 μM.

HP590 is an orally active, novel and potent STAT3 inhibitor (STAT3 luciferase activity: IC50=27.8 nM; ATP inhibition: IC50=24.7 nM). HP590 shows anti-proliferative activity to gastric cancer cells and induces apoptosis.