STAT Inhibitor

Morusin is a prenylated flavonoid isolated from Morus alba Linn. with various biological activities, such as antitumor, antioxidant, and anti-bacteria property. Morusin could inhibit NF-κB and STAT3 activity.

L-Glutamine-¹⁵N₂ is the ¹⁵N-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.

Delphinidin chloride is an anthocyanin isolated from berries and red wine. Delphinidin chloride exhibits endothelium-dependent vasodilation and anticancer activity. Delphinidin chloride also modulates JAK/STAT3 and MAPK signaling, thereby inducing apoptosis in HCT116 cells. Delphinidin chloride is also a potent inhibitor of EGFR (IC₅₀: 1.3 μM), shutting down downstream signaling cascades.

SI-109 is a potent STAT3 SH2 domain inhibitor (K_i=9 nM) with antitumor activity. SI-109 effectively inhibits the transcriptional activity of STAT3 (IC₅₀=3 μM). SI-109 and an analog of CRBN ligand lenalidomide have been used to design PROTAC STAT3 degrader SD-36.

Cilengitide TFA (EMD 121974 TFA) is an integrin (integrin) inhibitor with blood-brain barrier permeability, with IC₅₀ values against human targets as follows: 0.61 nM for αvβ3, 8.4 nM for αvβ5, 14.9 nM for α5β1, 5400 nM for αIIbβ3, 2050 nM for αvβ6, 2350 nM for αvβ8. Cilengitide TFA inhibits the binding of integrins to vitronectin, fibronectin, fibrinogen and LAP (TGF-β), and serves as an internal standard for solid-phase integrin binding assays. Cilengitide TFA inhibits tumor cell viability, induces apoptosis, reduces the phosphorylation levels of STAT3, AKT and mTOR, downregulates the expression of PD-L1, inhibits cell viability and angiogenesis, regulates anti-tumor immune responses and slows tumor growth. Cilengitide TFA can be used in research related to glioblastoma, melanoma, advanced solid tumors and refractory brain tumors.

SH-4-54 is a CNS-penetrant STAT inhibitor that binds to STAT3 and STAT5 with K_Ds of 300, 464 nM, respectively.

Cucurbitacin I is a natural selective inhibitor of JAK2/STAT3, with potent anti-cancer activity.

BP-1-102 is an orally available, small-molecule inhibitor of transcription factor Stat3, with an IC₅₀ of 6.8 μM.

Gondoic acid (cis-11-Eicosenoic acid), a monounsaturated long-chain fatty acid, is contained in a variety of plant oils and nuts. Gondoic acid can exert anti-inflammatory activity by inhibiting the production of ROS and the PKCθ/ERK/STAT3 signaling pathway. Gondoic acid can be used as a raw material for medical supplies and a moisturizing ingredient in cosmetic creams.

Anti-IL11 Antibody (X203) (EnX203) is a human-derived IgG1, κ type antibody inhibitor, targeting to human IL-11. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001).

Nitidine chloride, a potential anti-malarial lead compound derived from Zanthoxylum nitidum (Roxb) DC, exerts potent anticancer activity through diverse pathways, including inducing apoptosis, inhibiting STAT3 signaling cascade, DNA topoisomerase 1 and 2A, ERK and c-Src/FAK associated signaling pathway, also has anti-inflammatory activity. Nitidine chloride inhibits LPS-induced inflammatory cytokines production via MAPK and NF-kB pathway.

Anti-Mouse NK1.1 Antibody (PK136) is an anti-mouse NK1.1 IgG2a monoclonal antibody. Anti-Mouse NK1.1 Antibody (PK136) can deplete natural killer (NK) cells. Anti-Mouse NK1.1 Antibody (PK136) inhibits the JAK-STAT and NF-κB signaling pathways. Anti-Mouse NK1.1 Antibody (PK136) can be used for research on inflammation conditions such as non-alcoholic steatohepatitis (NASH).

STAT3-IN-1 (compound 7d) is an excellent, selective and orally active STAT3 inhibitor, with IC₅₀ values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 (compound 7d) induces tumor cells apoptosis.

L-Glutamine-¹⁵N is the ¹⁵N-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.

Guanosine 5'-diphosphate (GDP) sodium, 96% (HPLC) is a nucleoside diphosphate that activates adenosine 5'-triphosphate-sensitive K⁺ channel. Guanosine 5'-diphosphate sodium, 96% (HPLC) 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 sodium, 96% (HPLC) ameliorates the Turpentine-induced anemia of inflammation (AI) in mice when combined with FeSO₄. Guanosine 5'-diphosphate sodium, 96% (HPLC) can be used in the research of AI.

STAT6-IN-1 (Compound 19a) is a STAT6 inhibitor with a high affinity for the SH2 domain of STAT6 (IC₅₀=0.028 µM). STAT6-IN-1 can be used in studies of allergic lung disease, allergic rhinitis, chronic obstructive pulmonary disease or cancer.

Cardamonin can be found from cardamom, and can target various signaling molecules, transcriptional factors, cytokines and enzymes. Cardamonin can inhibit mTOR, NF-κB, Akt, STAT3, Wnt/β-catenin and COX-2. Cardamonin shows anticancer, anti-inflammatory, antimicrobial and antidiabetic activities.

Stapokibart (CM310) is a humanized monoclonal antibody targeting IL-4Rα (K_D values of 0.25 nM, 1.50 nM, and 2.75 nM for human, cynomolgus monkey, and rat IL-4Rα, respectively). Stapokibart effectively blocks the interaction of cytokines IL-4 and IL-13 with their co-receptor subunit IL-4Rα. Stapokibart reduces IL-4 and IL-13 mRNA, inhibits CD23 upregulation, and inhibits IL-4 and IL-13-induced STAT6 activation. Stapokibart improves inflammation (airway inflammation, rhinitis, dermatitis).

Casticin is a methyoxylated flavonol isolated from Vitex rotundifolia, with antimitotic and anti-inflammatory effect. Casticin inhibits the activation of STAT3.

Erasin is a potent Erlotinib (HY-50896)-resistance antagonizing STAT3 inhibitor with IC₅₀s of 9.7 and 24 μM against STAT3 and STAT1, respectively. Erasin induces cancer cells apoptosis.