STAT3 Inhibitor

ENMD-1198 (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-1198 is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization.

UC-514321, a structural analog of NSC370284 with higher activity, directly targets STAT3/5 and represses TET1 expression, but not TET2 or TET3. UC-514321 has the potential to treat acute myeloid leukemia (AML) both in vitro and in vivo, with low toxicity.

Momordicine I is a cucurbitane-type triterpenoids. Momordicine I suppresses glioma growth by promoting apoptosis and impairing mitochondrial oxidative phosphorylation. Momordicine I inhibits glycolysis, lipid metabolism, induces autophagy in HNC cells to suppress head and neck cancer growth. Momordicine I alleviates isoproterenol-induced cardiomyocyte hypertrophy through suppression of PLA2G6 and DGK-ζ. Momordicine I exerts its cardiovascular benefits by upregulating nitric oxide, inhibiting the activity of angiotensin-converting enzyme (ACE), activating the PI3K/Akt pathway, reducing oxidative stress and inflammation. Momordicine I inhibits AKT1, IL-6, and SRC, suggesting its potential application in type 2 diabetes.

Tofacitinib citrate (Standard) (Tasocitinib citrate (Standard); CP-690550 citrate (Standard)) is the analytical standard of Tofacitinib citrate (HY-40354A). This product is intended for research and analytical applications. Tofacitinib citrate (Tasocitinib citrate) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib citrate blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib citrate can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury.

SH5-07 is a hydroxamic acid based Stat3 inhibitor with an IC₅₀ of 3.9 μM in in vitro assay.

Phellodendrine is an orally active plant alkaloid. Phellodendrine inhibits the proliferation of KRAS-mutated pancreatic cancer cells by suppressing macropinocytosis and glutamine metabolism, inducing ROS accumulation and mitochondrial apoptosis. Phellodendrine promotes autophagy by activating the AMPK/mTOR pathway, alleviating intestinal damage in ulcerative colitis. Phellodendrine can alleviate gouty arthritis by inhibiting the IL-6/STAT3 signaling pathway. Phellodendrine suppresses allergic reactions by altering the conformation of MRGPRB3/MRGPRX2 protein, thereby inhibiting the activation of PKC and subsequent downstream MAPK and NF-κB signaling. Phellodendrine inhibits the AKT/NF-κB pathway and down-regulates the expression of COX-2, thereby protecting zebrafish embryos from oxidative stress. Phellodendrine has an anti-major depressive disorder (MDD) effect by down-regulating CHRM1, HTR1A, and the PI3K/Akt signaling pathway.

SD-1029 is a JAK2/STAT3 inhibitor. SD-1029 inhibits STAT3 nuclear translocation. SD-1029 is an inhibitor of STAT3 activation due to inhibition of JAK2 phosphorylation.

Galiellalactone is a is a small non-toxic and non-mutagenic fungal metabolite, a selective inhibitor of STAT3 signaling, with an IC₅₀ of 250-500 nM. Galiellalactone can be used to research castration-resistant prostate cancer.

Cyclanoline chloride is an alkaloid. Cyclanoline chloride can be isolated from Fangji. Cyclanoline (chloride) inhibits the phosphorylation of JAK2 and STAT3, and induces Apoptosis. Cyclanoline chloride suppresses tumor growth in subcutaneous bladder cancer xenograft models of nude mice. Cyclanoline chloride reverses cisplatin resistance in bladder cancer cells and enhances the efficacy of Cisplatin (HY-17394). Cyclanoline chloride can be used for research related to bladder cancer.

15 (R)-Lipoxin A4 (15-epi-LXA4) is a specialized pro-resolving mediator and an acetylated derivative of COX2. 15 (R)-Lipoxin A4 is present in neurons. 15 (R)-Lipoxin A4 induces the SPM synthases ALOX12 and ALOX15, as well as the pro-resolving receptor ALX. 15 (R)-Lipoxin A4 inhibits protein kinases, including JNK1/2/3, Lyn, STAT-3 and STAT-6. 15 (R)-Lipoxin A4 enhances the release of pro-resolving mediators. 15 (R)-Lipoxin A4 alleviates the pro-inflammatory phenotype of tendon-derived stromal cells. 15 (R)-Lipoxin A4 promotes the resolution of neuroinflammation. 15 (R)-Lipoxin A4 is applicable to research related to achilles tendinitis, achilles tendon rupture and Alzheimer’s disease.

Globulol is a terpenoid metabolite and Antimicrobial agent. Globulol can be isolated from Alpinia oxyphylla Miq. Globulol binds to PAK4, reduces the expression level of PAK4 in cancer cells, decreases the phosphorylation of AKT, and downregulates the expressions of STAT3, phosphorylated STAT3, and PD-L1. Globulol promotes the secretion of CCL4 by cancer cells. Globulol reduces the viability and proliferation ability of cancer cells, induces G0/G1 cell cycle arrest and Apoptosis in cancer cells, and inhibits cancer cell migration and the integrity of 3D tumor spheres. Globulol enhances the relevant effects of anti-PD-1 agents in the cancer cell microenvironment. Globulol exhibits anticancer activity against liver cancer. Globulol inhibits the mycelial growth of phytopathogenic fungi and the growth of phytopathogenic bacteria. Globulol can be used in studies related to hepatocellular carcinoma.

DCZ3301 is an apoptosis inducer. DCZ3301 modulates JAK2/STAT3, ERK1/2, and PI3K/AKT pathways. DCZ3301 induces G2/M and M phase cell cycle arrest and inhibits cell proliferation and viability. DCZ3301 enhances DNA damage, inhibits DNA repair, and suppresses angiogenesis. DCZ3301 can be used for the research of diffuse large B-cell lymphoma, multiple myeloma and leukemia/lymphoma.

STAT3-IN-37 (Compound 101) is the inhibitor for STAT3 with an IC₅₀ of 15 nM (measuring by DNA-HTRF assay) or 2 nM (measuring by human whole blood SOCS3 qPCR assay).

Pimozide-d₄ is a deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with K_is of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a K_i of 39 nM; Pimozide also inhibits STAT3 and STAT5.

Isocryptotanshinone is a dual STAT3 and PTP1B (IC₅₀ = 56.1 μM) inhibitor. Isocryptotanshinone inhibits STAT3 by binding to the STAT3 SH2 domain to block phosphorylation and nuclear translocation^[1][2]. Isocryptotanshinone exerts its anti-proliferative effect via the induction of cell cycle arrest, apoptosis, and pro-death autophagy, through the regulation of STAT3, AKT/mTOR and MAPK signaling pathways. Isocryptotanshinone suppresses the xenograft gastric cancer (GC) tumor growth in BALB/c nude mice. Isocryptotanshinone can be used for cancer research, such as lung cancer, breast cancer and GC.

INCA033989 is a fully human IgG1 monoclonal antibody targeting mutCALR (K_D = 1.75 nM for mutCALR^del52; K_D = 6.78 nM for mutCALR^ins5). INCA033989 antagonizes mutCALR-driven signaling and proliferation. INCA033989 selectively inhibits pSTAT3/pSTAT5. INCA033989 prevents thrombocytosis and reduces the expansion of mutCALR-positive cells. INCA033989 is useful for research on myeloproliferative neoplasms .

Guanosine 5'-diphosphate (GDP) is a nucleoside diphosphate that activates adenosine 5'-triphosphate-sensitive K⁺ channel. Guanosine 5'-diphosphate is an iron mobilizer, which forms a complex with hepcidin to inhibit the hepcidin-ferroportin (FPN) interaction and modulates the IL-6/stat-3 pathway. Guanosine 5'-diphosphate ameliorates the Turpentine-induced anemia of inflammation (AI) in mice when combined with FeSO₄. Guanosine 5'-diphosphate can be used in the research of AI.

HJC0123 is a STAT3 inhibitor. HJC0123 inhibits the proliferation of hepatic stellate cells and induces cell cycle arrest and apoptosis. HJC0123 reduces the phosphorylation, nuclear translocation and transcriptional activities of STAT3, increases the production of IL-6, inhibits the phosphorylation of Smad2/3 and down-regulates SOCS3. HJC0123 can be used in the study of liver fibrosis.

Golotimod (SCV-07), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod (SCV-07) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod (SCV-07) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).

ROCK2-IN-12 (Compound A25) is a selective ROCK2 inhibitor with an IC₅₀ of 7.0  nM for ROCK2 over ROCK1. ROCK2-IN-12 has potent antifibrotic effects via the TGF-β/Smad and ROCK2/STAT3 signaling pathways. ROCK2-IN-12 significantly reduces collagen deposition and reverses fibrotic progression in Bleomycin (HY-108345)-induced pulmonary fibrosis (PF) mouse models. ROCK2-IN-12 can be used for lung diseases like pulmonary fibrosis research.