Catalog No.
Product Name
Application
Product Information
Citations
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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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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
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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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
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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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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. - 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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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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STAT5 Degrader
AK-2292 is a potent and selective degrader of the STAT5 transcription factor, exhibiting a DC50 of 0.10 μM. This compound effectively induces the degradation of STAT5A/B proteins both in vitro and in vivo, demonstrating potential for tumor regression in acute myeloid leukemia and chronic myeloid leukemia xenograft mouse models. Additionally, AK-2292 features an alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions with azide-containing molecules, making it a valuable tool for chemical biology applications. -
STAT3/NF-κB Inhibitor
Triacetylresveratrol is an acetylated analog of Resveratrol that functions as an inhibitor of STAT3 and NF-κB signaling pathways. It effectively reduces the phosphorylation levels of STAT3 and NF-κB in a dose- and time-dependent manner in PANC-1 and BxPC-3 cancer cell lines. Its promising anticancer activity makes it a valuable tool for research in cancer biology and therapeutic development. -
Antihelminthic Agent
Niclosamide (BAY2353) is an orally active antihelminthic agent used in parasitic infection research. Niclosamide is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells. Niclosamide has biological activities against cancer, inhibits DNA replication in Vero E6 cells. -
PTPN1/PTPN2 Inhibitor
Osunprotafib (ABBV-CLS-484) is an orally active and selective active site PTPN1 (IC50: 2.5 nM) and PTPN2(IC50: 1.8 nM) inhibitor. Osunprotafib has 6-8-fold weaker activity on PTPN9 and no detectable activity on SHP-1 or SHP-2. Osunprotafib increases the sensitivity of human cancer cell lines to IFNγ. Osunprotafib generates robust anti-tumor immunity by enhancing JAK-STAT signalling and reducing T cell dysfunction. -
STAT3 Inhibitor
Pentadecanoic acid is a saturated fatty acid that serves as an inhibitor of STAT3, a critical transcription factor involved in cellular signaling pathways. Its primary biological activity includes modulation of inflammatory responses and potential anti-cancer effects. This compound is utilized in research applications focused on cancer therapy, inflammation studies, and metabolic regulation. -
STAT3 Inhibitor
STAT3-IN-13 is a potent inhibitor of the STAT3 signaling pathway, specifically targeting the SH2 domain with a binding affinity of 0.46 μM. This compound effectively inhibits the phosphorylation of STAT3 at Y705, subsequently reducing the expression of downstream target genes. In vitro studies demonstrate its ability to induce apoptosis, while in vivo applications show suppression of tumor growth and metastasis. STAT3-IN-13 is a valuable tool for cancer research, particularly in studies focused on the modulation of aberrant STAT3 activity. -
STAT3 Inhibitor
Atiprimod hydrochloride is a potent inhibitor of the signal transducer and activator of transcription 3 (STAT3). It demonstrates significant antitumor, anti-inflammatory, and anti-angiogenic properties by blocking IL-6 and VEGF signaling pathways, inhibiting the phosphorylation of JAK2 and JAK3. Atiprimod effectively induces cell cycle arrest, autophagy, and apoptosis in various cancer cell types, particularly through the activation of the PERK/eIF2α/ATF4/CHOP pathway in breast cancer cells. Its efficacy in tumor xenograft mouse models underscores its potential for investigating therapeutic approaches in conditions such as pituitary adenoma, breast cancer, multiple myeloma, and acute myeloid leukemia (AML). -
STAT3 Inhibitor
Atiprimod dimaleate is a selective inhibitor of the transcription factor STAT3, demonstrating significant antitumor, anti-inflammatory, and anti-angiogenic properties. By disrupting IL-6 and VEGF signaling pathways, it inhibits the phosphorylation of JAK2 and JAK3, effectively blocking the JAK-STAT signaling cascade. Atiprimod dimaleate induces cell cycle arrest, promotes autophagy and apoptosis, and activates the PERK/eIF2α/ATF4/CHOP pathway to trigger ER stress-mediated apoptosis in cancer cells. This reagent is valuable for research related to breast cancer, pituitary adenoma, multiple myeloma, and acute myeloid leukemia (AML), and has shown promising anti-tumor activity in xenograft mouse models. -
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.
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PROTAC CDK8-cyclin C dual degrader
LL-K8-22 is a potent, selective, and durable PROTAC degrader targeting the CDK8–cyclin C complex, with DC₅₀ values of 2.52 μM and 2.64 μM, respectively. It suppresses STAT1 Ser727 phosphorylation and inhibits E2F- and MYC-driven oncogenic transcriptional programs. LL-K8-22 shows potential for use in triple-negative breast cancer (TNBC) research and related therapeutic studies. -
PROTAC STAT3 Degrader
SD-36 is a selective PROTAC degrader of STAT3 that induces potent degradation of STAT3 protein both in vitro and in vivo, with minimal impact on other STAT family members. By suppressing STAT3-driven transcriptional programs, SD-36 inhibits the proliferation of acute myeloid leukemia and anaplastic large-cell lymphoma cells through cell cycle arrest and apoptosis. In xenograft mouse models, SD-36 achieves complete and sustained tumor regression at well-tolerated doses, making it a promising tool for cancer research and targeted therapy development. -
STAT1/3 Inhibitor
STAT1/3-IN-1 is a potent inhibitor of STAT1 and STAT3, targeting the phosphorylation and nuclear translocation of these transcription factors. This compound demonstrates significant anti-inflammatory activity by reducing LPS-induced production of pro-inflammatory cytokines such as NO, IL-1β, IL-6, and TNF-α, as well as inflammatory mediators like iNOS and COX-2. STAT1/3-IN-1 exhibits low toxicity in murine models, making it a valuable tool for investigating neuroinflammation and its underlying mechanisms. -
p-STAT3 Inhibitor
STAT3-IN-48 is a potent inhibitor of phosphorylated STAT3 (p-STAT3), functioning as a Sorafenib analogue. It effectively induces apoptosis in cancer cells through the inactivation of STAT3 via a SHP-1 dependent mechanism. Notably, STAT3-IN-48 does not inhibit general kinase activity, highlighting its specificity. This reagent is suitable for research applications focused on cancer biology and targeting STAT3 signaling pathways. -
STAT3/5 Inhibitor
UC-514321 is a potent inhibitor of STAT3 and STAT5, effectively repressing TET1 expression without affecting TET2 or TET3. This compound demonstrates significant promise for the treatment of acute myeloid leukemia (AML) in both in vitro and in vivo settings. Its selective action and low toxicity profile make it a valuable tool for research in cancer therapeutics. -
STAT3 inhibitor
C188 is a selective STAT3 inhibitor that disrupts STAT3 SH2/pY-peptide binding and inhibits IL-6-mediated STAT3 phosphorylation, with an IC50 of 20 µM. This compound effectively prevents the nuclear-to-cytoplasmic translocation of STAT3, thereby promoting apoptosis in breast cancer cell lines exhibiting constitutive STAT3 activation. C188 demonstrates potent biological activity with EC50 values of 0.73 µM, 3.96 µM, and 7.01 µM in MDA-MB-468, MDA-MB-231, and MDA-MB-435 cultures, respectively, highlighting its potential applications in cancer research. -
STAT3 Inhibitor
W1131 is a potent inhibitor of signal transducer and activator of transcription 3 (STAT3), which plays a critical role in oncogenic processes. By inducing ferroptosis, W1131 effectively suppresses cancer progression in various models, including gastric cancer subcutaneous xenografts, organoids, and patient-derived xenografts (PDX). Additionally, W1131 enhances chemosensitivity of cancer cells to 5-fluorouracil (5-FU), while modulating cell cycle dynamics, DNA damage response, and oxidative phosphorylation via the IL6-JAK-STAT3 and ferroptosis pathways. This compound is valuable for research into cancer biology and therapeutic resistance. -
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. - 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). -
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.
