STAT Inhibitor

Anti-Mouse CD106/VCAM-1 Antibody (M/K-2.7) is an anti-mouse CD106/VCAM-1 IgG1 monoclonal antibody. Anti-Mouse CD106/VCAM-1 Antibody (M/K-2.7) reduces inflammatory response and oxidative stress by lowering p-STAT3 and reactive oxygen species (ROS) levels. Anti-Mouse CD106/VCAM-1 Antibody (M/K-2.7) can alleviate cardiac inflammation and fibrosis by reducing the expression of collagen I and collagen III. Anti-Mouse CD106/VCAM-1 Antibody (M/K-2.7) can be used for research on cardiovascular conditions such as hypertensive heart condition and subretinal fibrosis.

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.

Lasiokaurin is an anticancer agent. Lasiokaurin can be isolated from Rabdosia rubescens (Hemsl.) H. Hara. Lasiokaurin inhibits the function of the PDPK1-AKT axis, with a K_d value of 75.93 μM for PDPK1. Lasiokaurin inhibits mTOR, STAT3, MAPK and NF-κB. Lasiokaurin reduces the mRNA and protein expression levels of PLK1. Lasiokaurin decreases DNA synthesis levels, induces cell Apoptosis, and regulates Autophagy processes. Lasiokaurin inhibits tumor growth in xenograft models. Lasiokaurin can be used in research related to nasopharyngeal carcinoma, triple-negative breast cancer.

STAT3-IN-12 is a potent STAT3 signal inhibitor that can inhibit IL-6 induced JAK/STAT3 signalling pathway activation. STAT3-IN-12 inhibits cancer cell growth, migration, and induce cell apoptosis as well as cycle arrest. STAT3-IN-12 can be used in cancer-related research, such as hepatocellular carcinoma (HCC) and oesophageal carcinoma.

UNC1062 is a highly selective tyrosine kinase (MERTK) inhibitor with an IC₅₀ of 1.1 nM (Morrison K_i = 0.33 nM). UNC1062 exhibits good selectivity for the TAM family (TYRO3 IC₅₀ = 60 nM, AXL IC₅₀ = 85 nM). UNC1062 exhibits significant anti-proliferative effects and induces apoptosis in various cancer models (such as melanoma, gastric cancer, and acute myeloid leukemia). UNC1062 inhibits multiple pathways, including MAPK/ERK, PI3K/AKT and JAK/STAT and affects the motility of head and neck squamous cell carcinoma (HNSCC) cells through the RhoA signaling pathway. UNC1062 inhibits macrophage efferocytosis, and it suitable for research on atherosclerosis.

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..

Ac-GpYLPQTV-NH2 acetate is a STAT3 inhibitor with an IC₅₀ value of 0.33 μM. Ac-GpYLPQTV-NH2 acetate has 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.

Picroside I is the major ingredient of Picrorhiza scrophulariiflora. Picrorhiza scrophulariiflora is a high value medicinal herb due to rich source of hepatoprotective metabolites, Picroside-I and Picroside-II. Picroside I is a promising agent for the management of asthma. Picroside I reduces the inflammation significantly at its higher dose. Picroside I also downregulates pSTAT6 and GATA3 expressions. Picroside I dose-dependently increases the serum levels of IFN-γ.

RSVA405 is a potent, orally active activator of AMPK, with an EC₅₀ of 1 μM. RSVA405 facilitates CaMKKβ-dependent activation of AMPK, inhibits mTOR, and promotes autophagy to increase Aβ degradation. RSVA405 has anti-inflammatory effects through the inhibition of STAT3 function. RSVA405 can also be used for the research of obesity.

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.

Desmethoxyyangonin is one of the six major kavalactones found in the Piper methysticum (kava) plant. Desmethoxyyangonin is a selective inhibitor of monoamine oxidase-B (MAO-B) (IC₅₀: 0.123  µM). Desmethoxyyangonin exerts anti-inflammatory effects by inhibiting Jak2/STAT3 and IKK signaling pathways. Desmethoxyyangonin induces CYP3A23 expression and leads to skeletal muscle relaxation.

Carabrone is a sesquiterpene found in the fruits of Carpesium abrotanoides and acts as a STAT3 inhibitor (K_d = 25.23 nM) with antibacterial, antitumor, and orally active properties. Carabrone covalently binds to UBE2D3 via Cys85 (K_d = 3.85 μM) and inhibits IκBα phosphorylation and NF-κB signaling. Carabrone induces ROS accumulation, loss of mitochondrial membrane potential, DNA fragmentation, and metacaspase-1-mediated apoptosis in fungi. Carabrone ameliorates autoimmune encephalomyelitis and MASH in vivo, reduces pro-inflammatory cytokines without immunotoxicity. Carabrone is used in research related to autoimmune encephalomyelitis, steatohepatitis, and fungal infections.

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.

JAK-IN-23 is an orally active double inhibitor of JAK/STAT and NF-κB. JAK-IN-23 can inhibit JAK1/2/3 with IC₅₀ values of 8.9 nM, 15 nM and 46.2 nM, respectively. JAK-IN-23 has potent inhibitory activities against interferon-stimulated genes (ISG) and NF-κB pathways with IC₅₀ values of 3.3 nM and 150.7 nM, respectively. JAK-IN-23 has great anti-inflammatory that decreases the release of various proinflammatory factors. JAK-IN-23 can be used for the research of inflammatory bowel disease (IBD).

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.

(DHQD)2PHAL (C-61) is a SYK tyrosine kinase inhibitor. (DHQD)2PHAL blocks SYK-dependent STAT3 signaling and prevents oxidative stress-induced STAT3 tyrosine phosphorylation and DNA-binding activity. (DHQD)2PHAL promotes oxidative stress-induced apoptosis. (DHQD)2PHAL can be used in research on B-cell precursor leukemia and B-lineage acute lymphoblastic leukemia.

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.