STAT3-IN-13 (compound 6f) is a STAT3 inhibitor. It exhibits anti-proliferative activity and binds to the STAT3 SH2 domain with a KD of 0.46 μM. This compound inhibits STAT3 Y705 phosphorylation and downstream target gene expression. In vitro studies show STAT3-IN-13 induces apoptosis, while in vivo experiments demonstrate its ability to suppress tumor growth and metastasis. STAT3-IN-13 has potential applications in cancer research.

STAT3-IN-12 is a potent inhibitor of STAT3signaling, by effectively blocking IL-6-induced activation of the JAK/STAT3 pathway. STAT3-IN-12 suppresses cancer cell proliferation and migration, while promoting apoptosis and inducing cell cycle arrest.

SGK1-IN-9 (Compound 1) is a SGK1 inhibitor. SGK1-IN-9 can be used in cancer research.

GRM1 modulator-1 is a GRM1 modulator.

DHX9-IN-21 (Compound 635) is a DHX9 inhibitor with an IC50 of 2 nM; its EC50 at the cellular level is 19.1 nM. DHX9-IN-21 exhibits antiproliferative activity against LS411N (CRC-MSI-H), with an IC50 value of 79.2 nM. DHX9-IN-21 can be used for the research of microsatellite unstable colorectal cancer.

CTR/AMYR modulator-1 is a calcitonin receptor/amylin receptor modulator. CTR/AMYR modulator-1 can be used for the research of metabolic disease.

Cathepsin L-IN-6 (Compound 6a) is a selective cathepsin L inhibitor with an IC50 of 0.021 μM. Cathepsin L-IN-6 suppresses cathepsin L activity by directly binding to cathepsin L. Cathepsin L-IN-6 inhibits IL-6 and IL-8. Cathepsin L-IN-6 shows a high anti-inflammatory activity. Cathepsin L-IN-6 can be used in the research of acute lung injury.

Anti-MRSA agent 36 (Compound III13) is an antibacterial agent with strong anti MRSA activity (MIC = 1 μg/mL). Anti-MRSA agent 36 targets phosphatidylglycerol (PG) on bacterial membranes, disrupting membrane integrity, leading to DNA leakage and increased ROS. Anti-MRSA agent 36 has advantages such as low cytotoxicity, low hemolysis, difficulty in inducing drug resistance, and good plasma stability. Anti-MRSA agent 36 can be used for the study of skin abscess and systemic infection models.

ALX-5407 ((R)-NFPS) is a selective and orally active glycine transporter GlyT1 inhibitor with an IC50 value of 3 nM. ALX-5407 can be used the research of N-methyl-D-aspartate-receptor function and schizophrenia.

YZ-35 is a STAT3 inhibitor, with a Ki value of 0.38 μM. YZ-35 binds directly to STAT3 with high affinity, exhibiting a dissociation constant (Kd) of 190 nM. YZ-35 directly attenuates the dual phosphorylation of STAT3 (Tyr705 and Ser727). YZ-35 suppresses colony formation, cellular migration, and induces apoptosis in breast cancer cell lines (BCSC). YZ-35 selectively suppresses BCSC self-renewal. YZ-35 inhibits tumor growth in the BCSC xenograft models. YZ-35 can be used for the study of breast cancer.

KB-15 is a STAT3 inhibitor. KB-15 exhibits potent anti-proliferative activity against AGS gastric cancer cells (IC50 = 0.29 μM) and BGC-823 gastric cancer cells (IC50 = 0.65 μM). KB-15 exerts anti-tumor effects by inhibiting STAT3 phosphorylation, downregulating HO-1 expression, and promoting intracellular ROS accumulation. KB-15 induces G0/G1 phase cell cycle arrest and apoptosis, as well as suppresses colony formation and migration of gastric cancer cells. KB-15 demonstrates excellent anti-tumor efficacy in BGC-823 subcutaneous xenograft model. KB-15 can be used for the study of gastric cancer.

STAT3 inhibitor N4 is a small molecule capable of inhibiting the STAT3 SH2 domain with IC50 of 0.57 uM, SPR KD of 1.04 uM, inhibits STAT3 dimerization and transcription in vitro and suppresses pancreatic cancer in vivo.N4 suppresses STAT3 activation in pancreatic cancer cells, suppresses pancreatic cancer cell growth, migration, and induces apoptosis.N4 (20 mg/kg, i.p.) suppresses pancreatic cancer growth, exhibits potent anti-metastatic activity in a pancreatic cancer liver metastasis mouse model, and prolongs survival of tumor-bearing mice.

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.