Catalog No.
Product Name
Application
Product Information
Citations
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STAT3 Inhibitor
STAT3-IN-10 is a selective inhibitor of the Signal Transducer and Activator of Transcription 3 (STAT3), exhibiting an IC50 value of 5.18 µM. This compound directly interacts with the SH2 domain of STAT3, leading to the induction of apoptosis in cancer cells. STAT3-IN-10 is ideal for research applications focused on elucidating STAT3 signaling pathways and exploring therapeutic strategies for cancer treatment. -
STAT3 Inhibitor
STAT3-IN-50 is a potent inhibitor of the Signal Transducer and Activator of Transcription 3 (STAT3) with an IC50 of 0.259 μM. This compound induces apoptosis and effectively inhibits the proliferation of colon and liver cancer cells. It is a valuable tool for research focused on the mechanisms of colon and liver cancers. -
STAT3 Inhibitor
HJC0152 (free base) is a potent and orally active inhibitor of STAT3. It effectively disrupts cell cycle progression and promotes apoptosis, making it a valuable tool for cancer research. Notably, HJC0152 (free base) demonstrates significant suppression of MDA-MB-231 xenograft tumor growth in murine models, indicating its potential utility in studying STAT3-related pathways in cancer. -
STAT5 Inhibitor
BP-1-108 is a selective inhibitor of STAT5, exhibiting a Ki value of 8.3 μM. This compound demonstrates significant anticancer activity by inducing apoptosis in leukemia cells through the inhibition of STAT5 phosphorylation. BP-1-108 is valuable for research applications focusing on acute myeloid leukemia and prostate cancer. -
JAK2/STAT3 Inhibitor
DPP is a Platinum(IV) complex featuring a pterostilbene-derived axial ligand that specifically targets the JAK2/STAT3 signaling pathway. This compound displays significant antiproliferative activity against breast cancer cells by inducing apoptosis through the activation of caspase-3 and cleavage of poly ADP-ribose polymerase. Additionally, DPP enhances the maturation and antigen presentation capability of dendritic cells, demonstrating favorable safety profiles in in vivo studies, making it a promising candidate for cancer immunotherapy research. -
STAT3 Inhibitor
HJC0416 is a potent inhibitor of STAT3, exhibiting significant antiproliferative activity and the ability to induce apoptosis. This compound effectively reduces the expression of phosphorylated STAT3 (Tyr-705) and Cyclin D1 while increasing the levels of cleaved caspase-3. HJC0416 demonstrates promising anti-tumor effects, making it relevant for cancer research applications focused on targeting the STAT3 signaling pathway. -
STAT3 Inhibitor
7-epi-Isogarcinol is a STAT3 inhibitor that exhibits moderate antiproliferative activity. By blocking the STAT3 signaling pathway, it effectively induces apoptosis and inhibits cell migration. This compound is valuable for research applications focused on cancer biology and the exploration of therapeutic strategies targeting STAT3-mediated pathways. -
JAK2/STAT3 Inhibitor
Cernuumolide J is a selective inhibitor of JAK2/STAT3 signaling pathway. It induces G2/M phase arrest and apoptosis in HEL leukemia cells by downregulating the phosphorylation of JAK2, STAT3, and Erk, while promoting the phosphorylation of JNK and p38 MAPK. Cernuumolide J exhibits a concentration-dependent growth inhibition of HEL leukemia cells, with an IC50 value of 1.79 μM, making it a valuable compound for research in anti-cancer therapy. -
STAT3 Inhibitor
STAT3-IN-52 is a selective inhibitor of signal transducer and activator of transcription 3 (STAT3) that acts by binding to the phosphorylated tyrosine 705 (pY705) site, with a Ki value of 440 nM. This compound effectively blocks the phosphorylation and dimerization of STAT3, leading to cytotoxic effects in various cancer cell lines, including MDA-MB-231 breast cancer cells (IC50 = 0.7 μM), UW426 medulloblastoma, and BKPC3 pancreatic cancer cells. Additionally, STAT3-IN-52 induces apoptosis, inhibits STAT3 nuclear transport and DNA binding, and downregulates the expression of the STAT3 target gene MMP9, making it a valuable reagent for studying STAT3 dysregulation in cancer research. -
IL6/STAT3 Inhibitor
Angoline is a selective inhibitor of the IL6/STAT3 signaling pathway, demonstrating an IC50 of 11.56 μM. It effectively inhibits the phosphorylation of STAT3, leading to reduced expression of target genes associated with cancer progression. This compound is valuable for research applications focused on cancer biology and the modulation of inflammatory responses. -
TYK2 Inhibitor
QL-1200186 is a selective, orally active allosteric inhibitor specifically targeting the pseudokinase domain JH2 of tyrosine kinase TYK2, exhibiting an IC50 of 0.06 nM with 164-fold selectivity over TYK1 JH2 (IC50 = 9.85 nM). By stabilizing the TYK2 JH2 conformation, QL-1200186 inhibits the activity of the JH1 catalytic domain and disrupts the IFNα, IL-12/IL-23-mediated JAK-STAT signaling pathway. This compound effectively reduces the production of Th1/Th17-related cytokines and has shown promise in alleviating skin inflammation in Imiquimod-induced psoriasis models, making it relevant for the study of autoimmune diseases such as psoriasis and systemic lupus erythematosus (SLE). -
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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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. -
STAT3 Inhibitor
LY5 is a potent inhibitor of STAT3, exhibiting an IC50 of 0.5 μM. It induces apoptosis and effectively inhibits STAT3 phosphorylation, demonstrating significant antitumor activity in vivo. This compound is utilized in cancer research to explore the mechanisms of STAT3-related signaling pathways and their implications in tumorigenesis. -
STAT3 Inhibitor
HJC0123 is a potent STAT3 inhibitor that effectively suppresses the proliferation of hepatic stellate cells while inducing cell cycle arrest and apoptosis. It reduces STAT3 phosphorylation, nuclear translocation, and transcriptional activity, leading to increased IL-6 production and inhibition of Smad2/3 phosphorylation, along with down-regulation of SOCS3. HJC0123 serves as a valuable tool for investigating liver fibrosis and related pathways. -
STAT3 Inhibitor
STAT3-IN-38 is a selective inhibitor of the signal transducer and activator of transcription 3 (STAT3) protein, exhibiting a KD value of 45.33 µM. By binding to the SH2 domain of STAT3, it effectively inhibits phosphorylation at the pTyr705 site, leading to the downregulation of downstream genes such as Survivin and Mcl-1. This compound has demonstrated the ability to block cell-cycle progression and induce apoptosis in colorectal cancer cells, making it a valuable tool for cancer research and therapeutic development. -
AKR1B1/STAT3/SLC7A11-Regulator
AKR1B1/STAT3/SLC7A11-regulator-1 is a regulatory compound that targets the AKR1B1, STAT3, and SLC7A11 pathways to enhance ferroptosis activity. This mechanism effectively reverses doxorubicin resistance in MCF-7/ADR breast cancer cells. It serves as a valuable tool in breast cancer research, particularly for studies focused on overcoming chemotherapy resistance and exploring ferroptosis as a therapeutic strategy. -
IKK/STAT3 Dual Inhibitor
ACHP is a selective IκB kinase (IKK) and STAT3 dual inhibitor, demonstrating potent inhibitory activity with IC50 values of 8.5 nM and 250 nM for IKKβ and IKKα, respectively. It effectively disrupts the STAT3 signaling pathway, leading to cancer cell cycle arrest and apoptosis. Additionally, ACHP exhibits significant anti-inflammatory properties in preclinical models, such as the mouse ear edema model. This compound is a valuable tool for research in anti-inflammatory and anti-cancer studies, including applications in multiple myeloma and leukemia. -
HDAC3/p-STAT3 Inhibitor
1-Stearoyl-sn-glycero-3-phosphocholine is an inhibitor of histone deacetylase 3 (HDAC3) and the phosphorylation of signal transducer and activator of transcription 3 (p-STAT3). This compound has demonstrated the ability to induce apoptosis and exhibits significant anticancer activity in chronic myelogenous leukemia (CML) K562 cells. It serves as a valuable tool for researchers investigating the therapeutic potential of HDAC inhibitors in cancer treatment. -
STAT3/JAK Inhibitor
Brevilin A is a potent inhibitor of the STAT3/JAK signaling pathway, with an IC50 value of approximately 10.6 μM for STAT3. It exhibits anti-tumor properties and effectively inhibits the proliferation of cancer cells. Additionally, Brevilin A has been shown to induce both apoptosis and autophagy, making it a valuable tool for cancer research and therapeutic investigations. -
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. -
EPAC1 Activator, STAT3 Modulator
DM243 is an EPAC1 activator and STAT3 modulator known for its ability to increase GTP-bound Rap1 levels specifically in EPAC1-expressing cells, while exhibiting no effects on EPAC2 or PKA. This compound effectively reduces IL-6/IL-6Rα-induced STAT3 phosphorylation in endothelial cells and suppresses TGF-β1-mediated fibroblast-to-myofibroblast transition, leading to decreased levels of α-smooth muscle actin and Collagen I in lung fibroblasts. Additionally, DM243 demonstrates minimal cytotoxicity in normal human lung fibroblasts, making it a valuable tool for studies related to fibrosis and inflammation. -
JAK/STAT Inhibitor
Phenylpyropene C is a JAK/STAT pathway inhibitor known to effectively inhibit interferon-gamma (IFN-γ) mediated expression of reporter genes, with an IC50 range of 5.4 to 10.8 μM. Additionally, it serves as an inhibitor of acyl-CoA, exhibiting an IC50 of 16.0 μM. This compound is valuable for research applications focusing on the modulation of immune responses and the exploration of cytokine signaling pathways. -
STAT6 Modulator
Medrysone, also known as 6α-Methyl-11β-hydroxyprogesterone, functions as a STAT6 modulator with significant implications for macrophage polarization. This compound enhances IL-4-induced STAT6 activation, leading to increased expression of M2 macrophage markers and elevated secretion of pro-angiogenic factors such as VEGF and CCL2. Additionally, Medrysone promotes the migratory capacity of M2-like macrophages towards endothelial cells, thereby facilitating tissue repair processes. Its efficacy in regulating macrophage polarization makes it a valuable tool for research on corneal injury and wound healing applications.
