Stat

BP-1-108 is a selective inhibitor of STAT5, exhibiting a Ki value of 8.3 μM. This compound demonstrates significant anticancer activity by inducing apoptosis in leukemia cells through the inhibition of STAT5 phosphorylation. BP-1-108 is valuable for research applications focusing on acute myeloid leukemia and prostate cancer.

DPP is a Platinum(IV) complex featuring a pterostilbene-derived axial ligand that specifically targets the JAK2/STAT3 signaling pathway. This compound displays significant antiproliferative activity against breast cancer cells by inducing apoptosis through the activation of caspase-3 and cleavage of poly ADP-ribose polymerase. Additionally, DPP enhances the maturation and antigen presentation capability of dendritic cells, demonstrating favorable safety profiles in in vivo studies, making it a promising candidate for cancer immunotherapy research.

HJC0416 is a potent inhibitor of STAT3, exhibiting significant antiproliferative activity and the ability to induce apoptosis. This compound effectively reduces the expression of phosphorylated STAT3 (Tyr-705) and Cyclin D1 while increasing the levels of cleaved caspase-3. HJC0416 demonstrates promising anti-tumor effects, making it relevant for cancer research applications focused on targeting the STAT3 signaling pathway.

7-epi-Isogarcinol is a STAT3 inhibitor that exhibits moderate antiproliferative activity. By blocking the STAT3 signaling pathway, it effectively induces apoptosis and inhibits cell migration. This compound is valuable for research applications focused on cancer biology and the exploration of therapeutic strategies targeting STAT3-mediated pathways.

Cernuumolide J is a selective inhibitor of JAK2/STAT3 signaling pathway. It induces G2/M phase arrest and apoptosis in HEL leukemia cells by downregulating the phosphorylation of JAK2, STAT3, and Erk, while promoting the phosphorylation of JNK and p38 MAPK. Cernuumolide J exhibits a concentration-dependent growth inhibition of HEL leukemia cells, with an IC50 value of 1.79 μM, making it a valuable compound for research in anti-cancer therapy.

STAT3-IN-52 is a selective inhibitor of signal transducer and activator of transcription 3 (STAT3) that acts by binding to the phosphorylated tyrosine 705 (pY705) site, with a Ki value of 440 nM. This compound effectively blocks the phosphorylation and dimerization of STAT3, leading to cytotoxic effects in various cancer cell lines, including MDA-MB-231 breast cancer cells (IC50 = 0.7 μM), UW426 medulloblastoma, and BKPC3 pancreatic cancer cells. Additionally, STAT3-IN-52 induces apoptosis, inhibits STAT3 nuclear transport and DNA binding, and downregulates the expression of the STAT3 target gene MMP9, making it a valuable reagent for studying STAT3 dysregulation in cancer research.

Angoline is a selective inhibitor of the IL6/STAT3 signaling pathway, demonstrating an IC50 of 11.56 μM. It effectively inhibits the phosphorylation of STAT3, leading to reduced expression of target genes associated with cancer progression. This compound is valuable for research applications focused on cancer biology and the modulation of inflammatory responses.

QL-1200186 is a selective, orally active allosteric inhibitor specifically targeting the pseudokinase domain JH2 of tyrosine kinase TYK2, exhibiting an IC50 of 0.06 nM with 164-fold selectivity over TYK1 JH2 (IC50 = 9.85 nM). By stabilizing the TYK2 JH2 conformation, QL-1200186 inhibits the activity of the JH1 catalytic domain and disrupts the IFNα, IL-12/IL-23-mediated JAK-STAT signaling pathway. This compound effectively reduces the production of Th1/Th17-related cytokines and has shown promise in alleviating skin inflammation in Imiquimod-induced psoriasis models, making it relevant for the study of autoimmune diseases such as psoriasis and systemic lupus erythematosus (SLE).

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.

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.

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.