Stat

Brevilin A is a potent inhibitor of the STAT3/JAK signaling pathway, with an IC50 value of approximately 10.6 μM for STAT3. It exhibits anti-tumor properties and effectively inhibits the proliferation of cancer cells. Additionally, Brevilin A has been shown to induce both apoptosis and autophagy, making it a valuable tool for cancer research and therapeutic investigations.

Iruplinalkib (WX-0593) is an orally active and selective ALK/ROS1 inhibitor that effectively blocks tyrosine autophosphorylation of ALK, mutant ALK, and EGFR, with IC50 values ranging from 5.38 to 16.74 nM. Additionally, it inhibits the transport activity of MATE1, MATE2K, P-gp, and BCRP. Iruplinalkib is under investigation for the treatment of non-small cell lung cancer (NSCLC).

Mogrol, a biometabolite of mogrosides, exerts its biological activity by inhibiting the ERK1/2 and STAT3 signaling pathways, suppressing CREB activation, and activating AMPK signaling.

STAT1/3-IN-1 is a potent inhibitor of STAT1 and STAT3, targeting the phosphorylation and nuclear translocation of these transcription factors. This compound demonstrates significant anti-inflammatory activity by reducing LPS-induced production of pro-inflammatory cytokines such as NO, IL-1β, IL-6, and TNF-α, as well as inflammatory mediators like iNOS and COX-2. STAT1/3-IN-1 exhibits low toxicity in murine models, making it a valuable tool for investigating neuroinflammation and its underlying mechanisms.

STAT3-IN-48 is a potent inhibitor of phosphorylated STAT3 (p-STAT3), functioning as a Sorafenib analogue. It effectively induces apoptosis in cancer cells through the inactivation of STAT3 via a SHP-1 dependent mechanism. Notably, STAT3-IN-48 does not inhibit general kinase activity, highlighting its specificity. This reagent is suitable for research applications focused on cancer biology and targeting STAT3 signaling pathways.

UC-514321 is a potent inhibitor of STAT3 and STAT5, effectively repressing TET1 expression without affecting TET2 or TET3. This compound demonstrates significant promise for the treatment of acute myeloid leukemia (AML) in both in vitro and in vivo settings. Its selective action and low toxicity profile make it a valuable tool for research in cancer therapeutics.

C188 is a selective STAT3 inhibitor that disrupts STAT3 SH2/pY-peptide binding and inhibits IL-6-mediated STAT3 phosphorylation, with an IC50 of 20 µM. This compound effectively prevents the nuclear-to-cytoplasmic translocation of STAT3, thereby promoting apoptosis in breast cancer cell lines exhibiting constitutive STAT3 activation. C188 demonstrates potent biological activity with EC50 values of 0.73 µM, 3.96 µM, and 7.01 µM in MDA-MB-468, MDA-MB-231, and MDA-MB-435 cultures, respectively, highlighting its potential applications in cancer research.

W1131 is a potent inhibitor of signal transducer and activator of transcription 3 (STAT3), which plays a critical role in oncogenic processes. By inducing ferroptosis, W1131 effectively suppresses cancer progression in various models, including gastric cancer subcutaneous xenografts, organoids, and patient-derived xenografts (PDX). Additionally, W1131 enhances chemosensitivity of cancer cells to 5-fluorouracil (5-FU), while modulating cell cycle dynamics, DNA damage response, and oxidative phosphorylation via the IL6-JAK-STAT3 and ferroptosis pathways. This compound is valuable for research into cancer biology and therapeutic resistance.

Phenylpyropene C is a JAK/STAT pathway inhibitor known to effectively inhibit interferon-gamma (IFN-γ) mediated expression of reporter genes, with an IC50 range of 5.4 to 10.8 μM. Additionally, it serves as an inhibitor of acyl-CoA, exhibiting an IC50 of 16.0 μM. This compound is valuable for research applications focusing on the modulation of immune responses and the exploration of cytokine signaling pathways.

DM245 is an EPAC1 activator and STAT3 phosphorylation inhibitor. It effectively increases Rap1-GTP levels through selective activation of EPAC1, without affecting EPAC2 or PKA. DM245 mitigates IL-6/IL-6Rα-mediated STAT3 phosphorylation in endothelial cells and inhibits the TGF-β1-induced transition of fibroblasts to myofibroblasts, leading to decreased levels of αSMA and Collagen I. Importantly, DM245 shows minimal cytotoxicity in normal human lung fibroblasts, indicating a high safety profile for extended exposure.

YN11 is a selective inhibitor of Signal Transducer and Activator of Transcription 3 (STAT3) with a Kd of 11.9 μM. By directly binding to the SH2 domain, YN11 effectively inhibits the phosphorylation of STAT3, leading to decreased expression of downstream target proteins. This compound has demonstrated significant biological activity, inducing cell cycle arrest and promoting apoptosis in prostate cancer cells, while also inhibiting cell invasion and migration. In vivo studies indicate that YN11 suppresses tumor growth in prostate cancer xenograft models without causing significant body weight loss or histopathological changes in major organs, making it a valuable tool for research in prostate cancer therapy.