STAT Inhibitor

Danvatirsen sodium (AZD9150 sodium) is an antisense oligonucleotide targeting STAT3. Danvatirsen sodium reduces the viability and promotes apoptosis of leukemia cell lines. Danvatirsen sodium inhibits the expression of endogenous STAT3 and its downstream target genes, and reduces the proliferation and tumorigenicity of neuroblastoma and lymphoma cells. Danvatirsen sodium inhibited tumor growth in mouse models of neuroblastoma, lymphoma, and non-small cell lung cancer. Danvatirsen sodium achieves STAT3 mRNA and protein depletion in a mouse model of epidermoid carcinoma. Danvatirsen sodium can be used in research related to lymphoma, myelodysplastic syndrome, acute myeloid leukemia, neuroblastoma and non-small cell lung cancer.

FLLL32, a synthetic analog of curcumina, is a JAK2/STAT3 dual inhibitor with anti-tumor activity. FLLL32 can inhibit the induction of STAT3 phosphorylation by IFNα and IL-6 in breast cancer cells.

SMI-10B13 is an Oncostatin M (OSM) inhibitor with a K_D of 6.6 μM. SMI-10B13 inhibits OSM-mediated STAT3 phosphorylation in T47D and MCF-7 cell lines (IC₅₀ = 136 and 164 nM, respectively). SMI-10B13 shows anti-tumor effect in human breast cancer mice models.

Curculigoside is the main saponin in C. orchioide, exerts significant antioxidant, anti-osteoporosis, antidepressant and neuroprotection effects. Curculigoside possesses significant anti-arthritic effects in vivo and in vitro via regulation of the JAK/STAT/NF-κB signaling pathway.

Notoginsenoside R2 (20(S)-Notoginsenoside R2; Ginsenoside Ng-R2) is an orally active notoginsenoside. Notoginsenoside R2 activates P90RSK and Nrf2 via the MEK1/2-ERK1/2 pathway to inhibit 6-OHDA-induced apoptotic damage in nerve cells. Notoginsenoside R2 upregulates SOX8/β-catenin by reducing miR-27a, thereby suppressing Aβ_25-35-induced neuronal apoptosis and inflammatory responses. Notoginsenoside R2 alleviates lipid accumulation and mitochondrial dysfunction in diabetic nephropathy by inhibiting c-Src. Notoginsenoside R2 alleviates hepatic fibrosis by inducing hepatic stellate cell senescence and inhibiting the inflammatory microenvironment via JAK/STAT3 suppression. Notoginsenoside R2 can be used in research related to Parkinson's disease, Alzheimer's disease, diabetic nephropathy and hepatic fibrosis.

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.

Cirsilineol, a natural flavone compound, selectively inhibits IFN-γ/STAT1/T-bet signaling in intestinal CD4⁺ T cells. Cirsilineol has potent immunosuppressive and anti-tumor properties. Cirsilineol significantly ameliorates trinitro-benzene sulfonic acid (TNBS)-induced T-cell-mediated experimental colitis in mice.

L-Glutamine-1-¹³C is the ¹³C-labeled L-Glutamine (HY-N0390). L-Glutamine is an orally active nutritional agent and cellular metabolism regulator. L-Glutamine is taken up in a Na⁺-dependent manner and targets multiple key molecules including glutaminase, mTORC1, NF-κB, STAT-3 and HIF-1α. L-Glutamine enhances glutaminolytic catabolism, drives the conversion of glutamate to α-ketoglutarate, thereby regulating gene expression, integrating metabolic signals, mediating glutamine flux and maintaining redox homeostasis. L-Glutamine also promotes cell proliferation, osteogenic differentiation and fracture healing, exerts neuroprotective and cardioprotective effects, and inhibits osteoarthritis. L-Glutamine can be applied to research related to osteoporosis, osteoarthritis, ischemic stroke and acute cantharidin-induced cardiotoxicity.

Angoline is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC₅₀ of 11.56 μM. Angoline inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.

5,6,7-Trimethoxyflavone is a flavonoid compound that can be isolated from plants Callicarpa japonica. 5,6,7-Trimethoxyflavone exhibits antiviral and anti-inflammatory activities through inhibition of NF-κB/AP-1/STAT signaling pathway.

5-FAM-GpYLPQTV-NH2 is a fluorescently labeled peptide and has STAT3 inhibitory activity. 5-FAM-GpYLPQTV-NH2 can be used in cancer research.

iHSP110-33 is an inhibitor for heat shock protein 110 (HSP110). iHSP110-33 exhibits antitumor efficacy agaisnt large B-cell lymphoma and classical Hodgkin lymphoma. iHSP110-33 shows a synergistic effect with Selinexor (HY-17536), inhibits the STAT6 phosphorylation, and enhances its antitumor activity..

Stafib-2 is a potent and selctive inhibitor of the transcription factor STAT5b, with an IC₅₀ of 82 nM and 1.7 μM for STAT5b and STAT5a, respectively. Stafib-2 exhibits poor cell permeability.

Arnicolide D is a sesquiterpene lactone that can be isolated from Centipeda minima. Arnicolide D is cytotoxic to tumor cells and can induce cell cycle arrest, apoptosis, and oncosis in tumor cells. Arnicolide D has anti-tumor activity.

Bruceantinol is a quassinoid that can be isolated from Brucea javanica, inhibits pepper mottle virus (PepMoV) in pepper. Bruceantinol is a STAT3 inhibitor demonstrating potent antitumor activity in in vitro and in vivo human colorectal cancer (CRC) models. Bruceantinol has potent anti-leukemic activity. Bruceantinol strongly inhibits STAT3 DNA-binding ability (IC₅₀ = 2.4 pM), blocks the constitutive and IL-6-induced STAT3 activation, and suppresses transcription of MCL-1, PTTG1, survivin and c-Myc. Bruceantinol binds with CDK2/4/6 to facilitate protein degradation through proteasome pathway. Bruceantinol can dose- and time-dependently reduces the cell growth, impede cell proliferation, disrupts the cell cycle, and induces necrosis in MCF-7 cells and apoptosis in MDA-MB-231 cells.

Peruvoside is a potent inhibitor of Src, PI3K, JNK, STAT, and EGFR. Peruvoside induces apoptosis and autophagy and possesses a broad spectrum of anticancer activity in breast, lung, liver cancers and leukemia. Peruvoside is a broad-spectrum and potent antiviral activity against positive-sense RNA viruses. Peruvoside sensitizes Gefitinib (HY-50895)-resistant tumour cells (A549, PC9/gef and H1975) to Gefitinib.

DZ2002 is an orally active, reversible and low-cytotoxic type III SAHH inhibitor (K_i=17.9 nM), with good immunosuppressive activity. DZ2002 prevents the development of experimental dermal fibrosis by reversing the profibrotic phenotype of various cell types. DZ2002 can be used in studies of autoimmune diseases such as lupus syndrome and systemic sclerosis.