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cytochrome oxidase inhibitor
Artesunate is a semisynthetic derivative of artemisinin used to treat malaria. It has also been shown to effective against other parasites such as liver flukes. Artesunate also demonstrates cytotoxic action against cancer cell lines of different tumor types. Artesunate has been shown to inhibit TNF--induced production of proinflammatory cytokines via inhibition of NF-B and PI3 kinase/Akt signal pathway in human rheumatoid arthritis fibroblast-like synoviocytes. -
Stat3 inhibitor
Cryptotanshinone, a natural compound isolated from the roots of Salvia miltiorrhiza Bunge (Danshen), dramatically blocks STAT3 Tyr705 phosphorylation but not STAT3 Ser727 phosphorylation in DU145 cells, and significantly inhibits JAK2 phosphorylation with IC50 of ~5 μM without affecting the phosphorylation of upstream kinases c-Src and EGFR. -
Pdia3/ERp57 activator, STAT3 inhibitor
Diosgenin is a steroid sapogenin and the precursor for the semisynthesis of progesterone which in turn was used in early combined oral contraceptive pills.It is the product of hydrolysis by acids, strong bases, or enzymes of saponins, extracted from the tubers of Dioscorea wild yam, such as the Kokoro.- Rashmi Rawat, .et al. , Food Chemistry Advances, 2022, 1: 100092
- Fludarabine or fludarabine phosphate (Fludara) is a chemotherapy drug used in the treatment of hematological malignancies (cancers of blood cells such as leukemias and lymphomas) .Fludarabine inhibits DNA synthesis by interfering with ribonucleotide reductase and DNA polymerase. It is active against both dividing and resting cells.
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STAT inhibitor
Fludarabine or fludarabine phosphate (Fludara) is a chemotherapy drug used in the treatment of hematological malignancies (cancers of blood cells such as leukemias and lymphomas) .Fludarabine inhibits DNA synthesis by interfering with ribonucleotide reductase and DNA polymerase. It is active against both dividing and resting cells.- Irene Dell'Anno, .et al. , Invest New Drugs, 2020, Dec 9 PMID: 33300108
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Stat3 Inhibitor
S3I-201 (NSC 74859) is a novel inhibitor of Stat3 that inhibits Stat3, Stat3 complex formation and Stat3-DNA binding activity in vitro (IC50 = 86 ?? 33 μM) and Stat3-dependent transcriptional activities.- Bae WJ, .et al. , J Exp Clin Cancer Res, 2019, 38:484 PMID: 31805999
- Ethan L. Morgan, .et al. , PLoS Pathog, 2018, Apr; 14(4): e1006975 PMID: 29630659
- Nishimura K, .et al. , Biochem Biophys Res Commun, 2018, Jan 1;495(1):1317-1321 PMID: 29191652
- Soleimani AH, .et al. , Drug Deliv Transl Res, 2017, Aug;7(4):571-581 PMID: 28290050
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multi-kinase inhibitor
Cenisertib (AS-703569) is a multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. -
multi-kinase inhibitor
Lestaurtinib (CEP-701;KT-5555) is a multi-kinase inhibitor with potent activity against the Trk family of receptor tyrosine kinases. Lestaurtinib inhibits JAK2, FLT3 and TrkA with IC50s of 0.9, 3 and less than 25 nM, respectively. -
STAT3 inhibitor
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 apoptosis.- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
- Rongshou Wu, .et al. , Sci Rep, 2023, 13: 16998 PMID: 37813900
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STAT3 inhibitor
Stattic is a small molecule shown to selectively inhibit the activation of the Stat3 transcription factor by blocking phosphorylation and dimerization events.- Siu Hong Dexter Wong, .et al. , Sci Adv, 2023, Jul 7;9(27):eadg9593 PMID: 37418519
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Pdia3/ERp57 activator, STAT3 inhibitor
Diosgenin glucoside, a saponin compound extracted from Tritulus terrestris L., provides neuroprotection by regulating microglial M1 polarization. Diosgenin glucoside protects against spinal cord injury by regulating autophagy and alleviating apoptosis . -
STAT inhibitor
Napabucasin is an orally-administered small molecule which can block cancer stem cell (CSC) self-renewal and induces cell death in CSCs as well as non-stem cancer cells. -
STAT Inhibitor
STAT5 Inhibitor is a cell-permeable, nonpetidic nicotinoyl hydrazone that suppresses STAT5 by targeting its SH2 domain (IC50 = 47 μM against STAT5?? SH2 domain EPO peptide binding activity). -
Stat3 inhibitor & Apoptosis inducer
Homoharringtonine is a cephalotaxine alkaloid which inhibits the formation of diphenylalanine and acetylphenylalanyl-puromycin in liver ribosomes. -
STAT inhibitor
Nitidine chloride, a natural benzophenanthridine alkaloid, has been shown to inhibit cancer growth via induction of cell apoptosis and suppression of cancer angiogenesis. -
JAK2/STAT3 inhibitor
Cucurbitacin I, Cucumis sativus L. has been found to suppress levels of phosphotyrosine Stat3 (signal transducer and activator of transcription 3) in v-Src-transformed NIH 3T3 cells. -
STAT3 inhibitor
Corylifol A is a phenolic compounds isolated from Psoralea corylifolia; inhibits IL-6-induced STAT3 activation and phosphorylation(IC50=0.8 uM). -
STAT inhibitor
Nifuroxazide is an inhibitor of STAT activation and signaling activity, is an oral nitrofuran antibiotic, used to treat colitis and diarrhea in humans and non-humans. -
STAT6 inhibitor
AS1517499 is a novel and potent STAT6 inhibitor with an IC50 value of 21 nM. - Balsalazide sodium hydrate could suppress colitis-associated carcinogenesis through modulation of IL-6/STAT3 pathway.
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anti-inflammatory agent
Balsalazide is an anti-inflammatory agent for treatment of Inflammatory Bowel Disease. Balsalazide could suppress colitis-associated carcinogenesis through modulation of IL-6/STAT3 pathway. -
STAT3 inhibitor
STAT3-IN-3 is a potent and selective inhibitor of signal transducer and activator of transcription 3 (STAT3). -
JAK2/STAT3 inhibitor
Protosappanin A is an immunosuppressive ingredient of the medicinal herb Caesalpinia sappan L. -
STAT3 inhibitor
inS3-54A18 is a potent STAT3 inhibitor, with anti-cancer properties. -
STAT5 inhibitor
STAT5-IN-2 is a STAT5 inhibitor with EC50s of 9 μM and 5 μM in K562 and KU812 cells, respectively. Potent antileukemic effect. -
AK-STAT3 signaling pathway inhibitor
Ganoderic acid A can inhibit of the JAK-STAT3 signaling pathway, also inhibit proliferation, viability, ROS. -
Pdia3/ERp57 activator, STAT3 inhibitor
Diosgenin palmitate, also known as Diosgenin hexadecanoate, is the hexadecanoic ester of Diosgenin. Diosgenin, a phytosteroid sapogenin, is the product of hydrolysis by acids, strong bases, or enzymes of saponins, extracted from the tubers of Dioscorea wild yam, such as the Kokoro. -
Colivelin TFA is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin TFA exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin TFA has the potential for the treatment of alzheimer's disease and ischemic brain injury.
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Colivelin is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin has the potential for the treatment of alzheimer's disease and ischemic brain injury
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IL-23 receptor antagonist
Icotrokinra (JNJ-77242113) is an orally available and selective antagonist of the interleukin-23 (IL-23) receptor. It potently inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC₅₀ = 5.6 pM) and suppresses IL-23-induced interferon-γ (IFN-γ) production in natural killer (NK) cells (IC₅₀ = 18.4 pM). Icotrokinra also demonstrates anti-inflammatory activity in a rat TNBS-induced colitis model. It is a promising therapeutic candidate for the study and treatment of inflammatory conditions such as psoriasis, psoriatic arthritis, and inflammatory bowel disease (IBD). - 6-Demethoxytangeretin is a flavonoid compound isolated from *Citrus reticulata* with demonstrated anti-inflammatory and anti-allergic properties. It inhibits IL-6 production and the expression of related genes in human mast cells by modulating the ALK and MAPK signaling pathways. Additionally, 6-Demethoxytangeretin enhances CRE-mediated transcription in hippocampal neurons, indicating potential neuroregulatory effects.
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ALK/ROS1 inhibitor
Iruplinalkib (WX-0593) is an orally active and selective ALK/ROS1 inhibitor that effectively blocks tyrosine autophosphorylation of ALK, mutant ALK, and EGFR, with IC50 values ranging from 5.38 to 16.74 nM. Additionally, it inhibits the transport activity of MATE1, MATE2K, P-gp, and BCRP. Iruplinalkib is under investigation for the treatment of non-small cell lung cancer (NSCLC). - Gondoic acid (cis-11-Eicosenoic acid) is a monounsaturated long-chain fatty acid found in various plant oils and nuts. It exhibits anti-inflammatory activity by reducing reactive oxygen species (ROS) production and inhibiting the PKCθ/ERK/STAT3 signaling pathway. Gondoic acid is also utilized as a raw material in medical applications and as a moisturizing agent in cosmetic formulations.

