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STAT3 Inhibitor
Eucannabinolide is a STAT3 inhibitor that targets the activation of STAT3 at tyrosine 705, inhibiting its translocation to the nucleus and reducing its DNA binding capacity. This compound demonstrates potential in studies related to triple-negative breast cancer (TNBC) and other diseases characterized by aberrant STAT3 signaling. Eucannabinolide serves as a valuable tool for researchers investigating therapeutic strategies aimed at modulating STAT3 pathways in oncogenesis. -
STAT3 Inhibitor
STAT3-IN-37 is a selective inhibitor of the transcription factor STAT3, exhibiting potent inhibitory activity with an IC50 of 15 nM in a DNA-HTRF assay and 2 nM in a human whole blood assay utilizing SOCS3 qPCR. This compound is valuable for research applications targeting STAT3-mediated signaling pathways, often implicated in oncogenesis and immune regulation. Its efficacy makes it a suitable tool for studies investigating the therapeutic potential of STAT3 modulation in cancer and inflammatory diseases. -
Hsp110-STAT3 Interaction Inhibitor
Hsp110-STAT3 PPI-IN-1 is a potent inhibitor of the Hsp110-STAT3 protein-protein interaction. This compound exhibits antiproliferative activity against the HPAEC cell line, demonstrating an IC50 value of 22.67 μM. It serves as a valuable tool for investigating the role of Hsp110-STAT3 interactions in various biological processes and therapeutic applications. -
STAT3 Inhibitor
S3I-1757 is a selective STAT3 inhibitor that effectively hinders the phosphorylation and dimerization of STAT3 proteins. By targeting this pathway, S3I-1757 demonstrates significant potential in the study of STAT3-driven malignancies, including melanoma. Its application is particularly relevant for investigating therapeutic strategies in cancers characterized by aberrant STAT3 activation. -
STAT3 Inhibitor
Ac-GpYLPQTV-NH2 is a selective inhibitor of the STAT3 signaling pathway, exhibiting an IC50 value of 0.33 μM. This compound demonstrates significant antitumor activity, making it a valuable tool for research in cancer biology and therapeutic applications targeting STAT3-mediated oncogenic functions. Its efficacy in modulating STAT3 activity provides insights into the role of this transcription factor in tumor progression and treatment resistance. -
STAT5a Inhibitor
Stafia-1-dipivaloyloxymethyl ester functions as a selective inhibitor of STAT5a. This compound effectively reduces the expression of phosphorylated STAT5a (pSTAT5a) in a concentration-dependent manner, demonstrating significant inhibition at doses ranging from 0-200 μM, while exhibiting minimal impact on phosphorylated STAT5b (pSTAT5b). Stafia-1-dipivaloyloxymethyl ester is valuable for research applications targeting STAT signaling pathways. -
STAT Inhibitor
Eupalinolide K is a selective STAT3 inhibitor derived from Eupatorium lindleyanum. This sesquiterpene lactone functions as a Michael reaction acceptor, demonstrating significant potential in modulating STAT3 signaling pathways. Its inhibitory activity makes Eupalinolide K useful in research related to cancer biology and inflammatory responses, providing insights into therapeutic strategies targeting the STAT3 pathway. -
STAT3 Inhibitor
STAT3-IN-7 is a potent inhibitor targeting Signal Transducer and Activator of Transcription 3 (STAT3). This aryl sulfonamido azetidine compound demonstrates significant anticancer properties, making it a valuable tool for research in cancer biology. It offers applications in studies aimed at elucidating the role of STAT3 signaling in tumor progression and therapeutic resistance. -
STAT3 Inhibitor
STAT3-IN-8 (compound H172) is a selective inhibitor of Signal Transducer and Activator of Transcription 3 (STAT3). It exhibits potent inhibitory activity against STAT3 signaling, which is often dysregulated in various cancers. This compound is valuable for cancer research, particularly in studies exploring the role of STAT3 in tumorigenesis and therapeutic interventions. -
STAT3 Inhibitor
HJC0149 is a selective inhibitor of signal transducer and activator of transcription 3 (STAT3), functioning by disrupting STAT3 signaling pathways. This compound exhibits potent biological activity, making it a valuable tool for research focused on cancer and inflammatory diseases where STAT3 plays a critical role in regulating cell proliferation and survival. Its efficacy positions HJC0149 as an essential reagent for investigating the therapeutic potential of STAT3 modulation in preclinical studies. -
STAT3 Inhibitor
STAT3-IN-29 is a selective inhibitor of Signal Transducer and Activator of Transcription 3 (STAT3). It demonstrates potent anti-proliferative effects on HaCaT cells with an IC50 value of 0.09 µM and has been shown to alleviate IMQ-induced psoriasis in mouse models. This compound is valuable for research aimed at understanding STAT3 signaling pathways and developing therapeutic strategies for psoriasis and other STAT3-related conditions. -
STAT3 Inhibitor
STAT3-IN-36 is a potent inhibitor of STAT3, with additional activity against LRPPRC and CDK1. This compound demonstrates significant anticancer effects, evidenced by its ability to inhibit HGC27 cells with an IC50 of 1.8 μM. STAT3-IN-36 serves as a valuable tool for research applications focused on cancer biology, particularly in elucidating the mechanistic roles of STAT3 and its associated pathways in tumor progression. -
STAT6 Inhibitor
STAT6-IN-11 is a selective inhibitor of the transcription factor STAT6, exhibiting an EC50 of 6 nM. It effectively reduces CCL17 secretion in peripheral human whole blood stimulated via the IL-13-IL-13 receptor/IL-4 receptor pathway, with an IC50 of 83 nM. This compound is valuable for research into dermatological and respiratory conditions, providing insights into the role of STAT6 in immune response and inflammation. -
STAT3 Inhibitor
Crispene E is a selective STAT3 inhibitor that effectively disrupts STAT3 dimerization with an IC50 of 10.27 μM. This compound demonstrates specific cytotoxicity towards STAT3-dependent MDA-MB-231 breast cancer cells, making it a valuable tool for studies investigating breast cancer pathways and potential therapeutic targets. Research applications include exploring the role of STAT3 in tumorigenesis and evaluating the efficacy of STAT3 inhibition in cancer treatment strategies. -
STAT3 Inhibitor
STAT3-IN-35 is a selective inhibitor of Signal Transducer and Activator of Transcription 3 (STAT3) that targets the SH2 domain. This compound effectively inhibits STAT3 phosphorylation, demonstrating significant antiproliferative effects in triple-negative breast cancer (TNBC) cell lines. Additionally, STAT3-IN-35 exhibits pronounced antitumor activity and toxicity in TNBC xenograft models, making it a valuable tool for cancer research and therapeutic development. -
STAT3 Inhibitor
STAT3-IN-47 is a potent oral inhibitor of the Signal Transducer and Activator of Transcription 3 (STAT3) pathway. This compound demonstrates significant anti-tumor activity across various cancer cell lines, including HeLa, HepG2, U87, and LN229. By effectively suppressing STAT3 activation in vitro, STAT3-IN-47 serves as a valuable tool for research on solid tumors, with particular relevance to central nervous system malignancies and hepatocellular carcinoma. -
STAT6 Inhibitor
STAT6-IN-8 is a selective inhibitor of the signal transducer and activator of transcription 6 (STAT6), known for its potential anti-inflammatory and anti-allergic properties. This compound serves as a valuable tool for investigating STAT6-associated pathologies, including various inflammatory conditions such as atopic dermatitis and bronchial asthma, as well as allergic diseases like allergic rhinitis and chronic sinusitis. Its applications in research can contribute to a better understanding of these conditions and aid in the development of targeted therapies. -
pSTAT3 Inhibitor
(E/Z)-OSM-SMI-10B is a potent inhibitor of phosphorylated STAT3 (pSTAT3). This compound effectively decreases OSM-induced STAT3 phosphorylation in cancer cells when co-incubated with Oncostatin M (OSM). Its ability to modulate STAT3 signaling makes (E/Z)-OSM-SMI-10B a valuable tool for research in cancer biology and therapeutic development. -
STAT3 Inhibitor
STAT3-IN-23 is a potent inhibitor of signal transducer and activator of transcription 3 (STAT3). By selectively targeting STAT3, this compound disrupts its signaling pathway, leading to decreased tumor cell proliferation and enhanced apoptosis. STAT3-IN-23 is valuable for research applications focused on cancer biology, inflammation, and the understanding of STAT3-mediated signaling in various pathological conditions. -
STAT3 Inhibitor
STAT3-IN-5 is a potent inhibitor of the signal transducer and activator of transcription 3 (STAT3), primarily targeting the phosphorylation of STAT3 at the Y705 residue with an EC50 of 170 nM. This compound effectively blocks cytokine-induced JAK activation and induces apoptosis in cancer cells. STAT3-IN-5 is valuable for research focused on cancer biology and the therapeutic modulation of the STAT3 signaling pathway. -
STAT3 Dual Phosphorylation Inhibitor
STAT3-IN-32 is a potent inhibitor of dual phosphorylation of STAT3, targeting the SH2 domain with a dissociation constant (KD) of 21.3 nM. It effectively inhibits STAT3 phosphorylation at tyrosine 705 and serine 727, leading to the disruption of nuclear transcription and mitochondrial oxidative phosphorylation functions. In cellular assays, STAT3-IN-32 demonstrates an IC50 of 5.3 nM for STAT3 luciferase activity in HEK293T cells and 4.2 nM for ATP production inhibition in BxPC-3 cells. Additionally, STAT3-IN-32 exhibits significant anti-tumor effects in pancreatic cancer xenograft models, making it a valuable compound for cancer research. -
STAT3 Inhibitor
WZ-2-033 is a selective inhibitor of Signal Transducer and Activator of Transcription 3 (STAT3). This compound effectively reduces the proliferation, colony survival, migration, and invasion of cancer cell lines MDA-MB-231, HCC70, and MDA-MB231-4175, with IC50 values of 0.7 μM, 1.3 μM, and 1.3 μM, respectively. Its ability to modulate STAT3 signaling makes WZ-2-033 a valuable tool in cancer research and therapeutic development targeting STAT3-mediated pathways. -
STAT3 Inhibitor
STAT3-IN-43 is a covalent inhibitor that targets the allosteric site at the intersection of the STAT3 coiled-coil domain and DNA-binding domain, demonstrating an IC50 of 40.7 μM. This compound effectively modulates STAT3 activity, making it a valuable tool in cancer research to study the role of STAT3 in tumorigenesis and therapeutic resistance. Its application may extend to elucidating the molecular mechanisms of STAT3-mediated signaling pathways. -
STAT3 Inhibitor
STAT3-IN-4 is a selective inhibitor of the Signal Transducer and Activator of Transcription 3 (STAT3) signaling pathway. With dissociation constants (Kd) of 22.75 μM for the mutant STAT3 (I634S/Q635G) and 4.59 μM for the wild-type, this compound demonstrates significant potential in attenuating STAT3 activity. STAT3-IN-4 has been shown to inhibit the proliferation of tumor cells, making it a valuable tool for cancer research and therapeutic studies targeting aberrant STAT3 signaling in various malignancies. -
AK/STAT Signaling Inhibitor
AUH-6-96 is a potent JAK/STAT signaling inhibitor that effectively reduces Unpaired-induced transcriptional activity in Drosophila cells and inhibits tyrosine phosphorylation of STAT92E. It also suppresses both constitutive and IL-6-induced phosphorylation of STAT3 while decreasing levels of tyrosine-phosphorylated JAK3. Furthermore, AUH-6-96 induces apoptosis in cancer cells by downregulating anti-apoptotic genes downstream of STAT3, selectively reducing the viability of cancer cells with dysregulated JAK/STAT signaling. This compound is relevant for research pertaining to Hodgkin's lymphoma, breast cancer, and prostate cancer. -
STAT3 Inhibitor
STAT3-IN-33 is a selective STAT3 inhibitor that demonstrates significant anti-cancer properties. It effectively inhibits cell proliferation in HCT116, MCF-7, and MDA-MB-231 cancer cell lines, with IC50 values of 6.44, 3.29, and 4.86 μM, respectively. This compound is valuable for research focused on the therapeutic applications of STAT3 inhibition in breast and colon cancer. -
STAT3 Inhibitor
STAT3-IN-30 is a selective inhibitor of Signal Transducer and Activator of Transcription 3 (STAT3) with an EC50 of 13.8 μM. This compound effectively impairs STAT3-mediated signaling pathways, thereby influencing cell proliferation and survival. STAT3-IN-30 is suitable for research applications focused on cancer biology, immune response, and chronic inflammatory disorders, providing valuable insights into therapeutic targets involving STAT3 dysregulation. -
STAT3 Inhibitor
inS3-54-A26 is a selective inhibitor of the Signal Transducer and Activator of Transcription 3 (STAT3) pathway. It exhibits cytotoxicity in non-cancerous lung fibroblasts with an IC50 of 4.0 μM. This compound is valuable for research applications in cancer biology and therapeutic development, particularly for exploring STAT3's role in oncogenesis and its potential as a target for anti-cancer strategies. -
STAT3 Inhibitor
STAT3-IN-15 is a selective inhibitor of STAT3, a transcription factor implicated in various pathological conditions, including idiopathic pulmonary fibrosis (IPF). This compound effectively inhibits STAT3 phosphorylation, leading to a reduction in migration and deformation of epithelial cells stimulated by TGF-β1. Additionally, STAT3-IN-15 demonstrates the ability to hinder epithelial-mesenchymal transition (EMT), making it a valuable tool for research in fibrosis and related cellular processes. -
STAT3 Inhibitor
Pulchinenoside E2 is a triterpene saponin that functions as a STAT3 inhibitor. It exhibits dual activity by inhibiting STAT3 and autophagy, demonstrating cytotoxic effects on HL-60 cells with an IC50 value of 2.6 µg/mL. This compound is valuable for research applications focused on cancer biology and the modulation of signaling pathways involved in cell proliferation and survival. -
STAT Phosphorylation Inhibitor
XZH-5 is a STAT phosphorylation inhibitor that specifically targets the phosphorylation of STAT3. This compound induces apoptosis in various cancer cell lines and significantly reduces their colony-forming ability. It serves as a valuable tool for researchers investigating the role of STAT3 in tumorigenesis and potential therapeutic strategies for cancer treatment. -
STAT3 Inhibitor
PMMB-187 is a selective inhibitor of the Signal Transducer and Activator of Transcription 3 (STAT3), showing an IC50 value of 1.81 μM in MDA-MB-231 breast cancer cells. This compound effectively induces apoptosis by disrupting STAT3's transcriptional activity and nuclear localization, leading to a decrease in downstream gene expression. Additionally, PMMB-187 diminishes mitochondrial membrane potential, increases reactive oxygen species (ROS) production, and upregulates apoptosis-related protein levels. Its unique mechanism positions PMMB-187 as a valuable tool in cancer research applications. -
IRS1/2/STAT3 Inhibitor
NT219 is a potent dual inhibitor of insulin receptor substrates 1 and 2 (IRS1/2) and signal transducer and activator of transcription 3 (STAT3). It disrupts IRS1/2 degradation and inhibits STAT3 phosphorylation, impacting essential signaling pathways associated with various oncogenic processes. NT219 is relevant for research applications focused on cancer biology, particularly in understanding the interplay of these critical signaling molecules in tumor progression and resistance. -
STAT3 Inhibitor
STAT3-IN-9 is a selective inhibitor of STAT3, specifically targeting its activation by preventing Tyr705 phosphorylation while leaving STAT1 (Tyr701) unphosphorylated. This compound demonstrates significant biological activity by inducing apoptosis and causing cell cycle arrest at the G2/M phase. It can be effectively utilized in research applications focusing on cancer biology and the role of STAT3 in tumor progression. -
STAT3 Inhibitor
STAT3-IN-53 is a selective inhibitor of STAT3, targeting its SH2 domain with a Kd value of 6.16 μM. This compound effectively suppresses phosphorylation at the Y705 site, thereby inhibiting the IL-6/JAK/STAT3 signaling pathway. By downregulating the transcription and expression of critical oncogenes such as cyclin D1 and c-Myc, STAT3-IN-53 induces cell cycle arrest and promotes apoptosis, demonstrating potential anticancer activity, particularly in colorectal cancer research applications. -
EGFR/HER2/TS Inhibitor
EGFR/HER2/TS-IN-1 is a selective inhibitor targeting EGFR, HER2, and thymidylate synthase (TS) with IC50 values of 0.203 μM, 0.088 μM, and 0.168 μM, respectively. This compound is effective in inducing apoptosis in MCF7 breast cancer cells, making it a valuable tool for cancer research. Its ability to simultaneously inhibit multiple targets renders it a promising candidate for exploring therapeutic strategies in malignancies characterized by overactive EGFR and HER2 signaling pathways. -
EGFR Inhibitor
EGFR-IN-150 is a potent inhibitor of the epidermal growth factor receptor (EGFR), effectively blocking phosphorylation of mutant EGFR and downstream AKT signaling, leading to antitumor activity. This compound demonstrates an IC50 of 0.386 μM in the non-small cell lung cancer (NSCLC) cell line H1975, significantly reducing colony formation and migration in both H1975 and A549 cells while promoting apoptosis. Furthermore, EGFR-IN-150 exhibits substantial tumor growth suppression in the H1975 cell-derived xenograft (CDX) mouse model, making it a valuable tool for research focused on non-small cell lung cancer. -
EGFR Inhibitor
Erbstatin is an inhibitor of the epidermal growth factor receptor (EGFR), targeting its kinase activity to impede downstream signaling pathways. This compound exhibits significant antineoplastic properties, making it a valuable reagent in cancer research. Erbstatin is utilized in studies investigating the role of EGFR in tumor progression and response to therapy, providing insights into potential treatment strategies for EGFR-mediated malignancies. -
JAK/HDAC Inhibitor
JAK/HDAC-IN-2 is a dual-target inhibitor of Janus kinase (JAK) and histone deacetylase (HDAC), specifically inhibiting HDAC3/6 and JAK1/2 with nanomolar potency. This compound demonstrates proapoptotic activity by inhibiting histone deacetylation and STAT3 phosphorylation, contributing to its mechanism of action. JAK/HDAC-IN-2 exhibits significant antiproliferative effects in various hematological malignancies and solid tumors, making it a valuable tool for cancer research and therapeutic studies. -
PIM-1/HDAC Inhibitor
PIM-1/HDAC-IN-1 is a selective inhibitor of PIM-1 as well as histone deacetylases HDAC 1 and HDAC 6, exhibiting an IC50 of 343.87 nM for PIM-1 and 63.65 nM and 62.39 nM for HDAC 1 and HDAC 6, respectively. This compound demonstrates significant apoptotic activity in MCF-7 cell lines, inducing pre-G1 apoptosis and causing cell cycle arrest at the G2/M phase. PIM-1/HDAC-IN-1 is a valuable tool for research on cancer biology and the regulation of cell proliferation and apoptosis. -
STAT3 Inhibitor
STAT3-IN-18 is a STAT3 inhibitor that selectively targets the JAK2-STAT3 signaling pathway, demonstrating significant anti-proliferative effects in breast cancer cells. This compound promotes apoptotic cell death through the activation of caspase-3 and increases cleaved polyADP-ribose polymerase levels. Additionally, STAT3-IN-18 enhances the maturation and antigen presentation of dendritic cells, while exhibiting favorable safety profiles in vivo, making it a valuable tool for cancer research and immunotherapy studies. -
EGFR2 Inhibitor
EGFR-IN-105 is a selective inhibitor of the EGFR2 receptor, with an IC50 value of 0.68 μM. This compound demonstrates significant anticancer activity by inducing apoptosis in cancerous cells, making it a valuable tool for investigating therapeutic strategies in pancreatic cancer research. Its specificity and potency position it as an important reagent for studies focused on targeting EGFR-related pathways in oncology. -
EGFR Inhibitor
EGFR-IN-45 is a potent inhibitor of the epidermal growth factor receptor (EGFR) with IC50 values of 0.4 µM for EGFR and 1.6 µM for CDK2. Additionally, it demonstrates inhibitory activity against Topoisomerase I and Topoisomerase II. This compound effectively induces apoptosis and arrests cancer cells in the pre-G1 phase, making it a valuable tool for cancer research and therapeutic studies targeting EGFR-related pathways. -
EGFR Inhibitor
Avitinib maleate dihydrate is a potent, irreversible, orally active selective inhibitor of epidermal growth factor receptor (EGFR). It exhibits high affinity, with IC50 values of 0.18 nM for both EGFR L858R and EGFR T790M mutations, as well as 7.68 nM for wild-type EGFR. In addition to its EGFR inhibition, Avitinib maleate dihydrate functions as a Bruton’s tyrosine kinase (BTK) inhibitor, promoting apoptosis in mantle cell lymphoma by inhibiting BTK phosphorylation. Its diverse targeting capabilities make it valuable for cancer research applications. -
EGFR Inhibitor
EGFR-IN-51 is a potent inhibitor of the epidermal growth factor receptor (EGFR), exhibiting IC50 values of 0.493 µM for wild-type EGFR, 102.60 µM for the L858R-TK mutation, and 461.63 µM for the T790M-TK mutation. This compound demonstrates significant cytotoxic activity against various cancer cell lines, effectively inducing apoptosis. EGFR-IN-51 is applicable in research focused on targeted cancer therapies and elucidating the role of EGFR signaling in tumorigenesis. -
JAK2/Bcr-Abl/FLT3 Inhibitor
LS-104 is a non-ATP-competitive inhibitor targeting JAK2, Bcr-Abl, and FLT3. It effectively induces apoptosis in JAK2V617F-positive cells while inhibiting JAK2 autophosphorylation and downstream signaling pathways. Additionally, LS-104 demonstrates significant cytotoxic effects and inhibits the proliferation of FLT3-expressing leukemic cells. This hydroxystyryl-acrylonitrile compound holds potential for research into myeloproliferative disorders and refractory or relapsed hematologic malignancies. -
EGFR Inhibitor
EGFR-IN-141 is a potent inhibitor of the epidermal growth factor receptor (EGFR), demonstrating an IC50 of 2.67 nM. This compound exhibits significant cytotoxicity in A549 lung cancer cells, with an IC50 of 13.75 μM. EGFR-IN-141 has been shown to induce apoptosis and cause mitochondrial membrane depolarization, highlighting its potential for antitumor efficacy in cancer research applications. -
JAK3 Inhibitor
PRN-371 is a potent and selective inhibitor of JAK3. By disrupting the JAK3-STAT signaling pathway, PRN-371 effectively suppresses the proliferation of natural killer and T-cell lymphoma cells, inducing apoptosis in these malignancies. This compound demonstrates significant antitumor activity and is applicable in the research of various cancer types, particularly hematological malignancies. -
JAK2 Inhibitor
JAK2-IN-14 is a highly selective JAK2 inhibitor with an IC50 of 2 nM, demonstrating significant selectivity with 89.5-fold over JAK1, 80.5-fold over JAK3, and 51-fold over TYK2. This compound effectively inhibits the STAT5 signaling pathway, leading to tumor cell cycle arrest and apoptosis. JAK2-IN-14 is a valuable tool for investigating myeloproliferative neoplasms (MPNs) and their underlying mechanisms. -
PIM1 Inhibitor
PIM1-IN-3 is a selective inhibitor of the PIM1 kinase, known for its role in promoting cell survival and proliferation. This compound effectively induces apoptosis in Colo320 cells, demonstrating its potential as a therapeutic agent in cancer research. PIM1-IN-3 serves as a valuable tool for studying PIM1-related signaling pathways and exploring targeted cancer treatments.

