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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
EGFR Inhibitor
EGFR-IN-172 is a selective epidermal growth factor receptor (EGFR) inhibitor that effectively disrupts the proliferation of non-small cell lung cancer (NSCLC) cells harboring L858R, T790M, and C797S drug-resistant mutations. This compound acts by inhibiting EGFR phosphorylation, leading to cell cycle arrest and apoptosis in affected cells. EGFR-IN-172 serves as a valuable tool for research focused on NSCLC treatment and the development of targeted cancer therapies. -
Pim-1 Inhibitor
Pim-1 kinase inhibitor 1 is a selective inhibitor of Pim-1 kinase, demonstrating an IC50 value of 0.11 μM. This compound exhibits significant anticancer activity across various cancer cell lines by promoting cellular apoptosis. Pim-1 kinase inhibitor 1 is a valuable tool for research applications focused on cancer biology and therapeutic development. -
Miticide/STAT3 Inhibitor
Fluacrypyrim is a potent miticide that functions as a selective inhibitor of the STAT3 signaling pathway. It effectively induces growth arrest and apoptosis in STAT3-dependent cancer cells by significantly decreasing cyclin D1 protein and mRNA levels, leading to G1 cell cycle arrest. Additionally, Fluacrypyrim mitigates irradiation-induced hematopoietic system injury by protecting hematopoietic stem cells from apoptosis. Its analgesic and anti-inflammatory properties are demonstrated through the inhibition of uterine smooth muscle contraction and inflammatory responses, making it a valuable reagent for cancer and inflammation research. -
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. -
JAK3 Inhibitor
NSC114792 is a selective inhibitor of Janus kinase 3 (JAK3), which plays a critical role in immune signaling pathways. This compound effectively induces apoptosis in target cells and significantly reduces the protein expression of phosphorylated JAK3 and phosphorylated STAT5. NSC114792 is primarily utilized in research focused on immune responses and related signaling cascades. -
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. -
Pan-Pim kinase Inhibitor
VS-II-173 is a potent pan-Pim kinase inhibitor, exhibiting IC50 values of 0.07 μM for Pim1 and 0.02 μM for Pim3, with a residual activity of 46% at 1 μM for Pim2. This compound selectively targets acute myeloid leukemia (AML) cells, demonstrating significant inhibition of key phosphorylation events, including Stat5 (Y694) and MDM2 (S166), which disrupts pro-survival signaling pathways and promotes apoptosis. VS-II-173 shows enhanced anti-AML efficacy when used in combination with Daunorubicin and is especially relevant for research involving AML characterized by FLT3-ITD and NPM1 mutations. Its minimal toxicity to non-malignant cells makes it a valuable tool in cancer research. -
EGFR/FAK Inhibitor
EGFR-IN-46 is a potent dual inhibitor targeting the epidermal growth factor receptor (EGFR) and focal adhesion kinase (FAK), with IC50 values of 20.17 nM and 14.25 nM, respectively. This compound effectively inhibits cancer cell proliferation and induces apoptotic pathways in these cells. EGFR-IN-46 is designed for research applications focused on cancer biochemistry and therapeutic development. -
EGFR Inhibitor
EGFR-IN-60 is a potent inhibitor of the epidermal growth factor receptor (EGFR), specifically targeting EGFRWT, EGFRT790M, EGFRL858R, and JAK3 with IC50 values of 83, 26, 53, and 69 nM, respectively. This compound effectively suppresses the proliferation of H1975 cells with the EGFRT790M mutation (IC50=1.32 µM) while yielding less potency against A431 cells expressing EGFRWT (IC50=4.96 µM). With favorable oral bioavailability, EGFR-IN-60 demonstrates significant antitumor activity, promoting cell death via apoptosis as indicated by an increased Bax/Bcl-2 ratio. This makes it a valuable candidate for research into targeted therapies for EGFR-related cancers. -
EGFR Inhibitor
EGFR-IN-62 is a potent and reversible inhibitor of the epidermal growth factor receptor (EGFR) kinase, demonstrating IC50 values of 10 nM for the L858R/T790M mutation, 29 nM for wild-type EGFR, and 242 nM for the L858R/T790M/C797S mutation. This compound exhibits significant antiproliferative effects on human lung cancer cell lines A549 and H1975, with IC50 values of 2.53 μM and 1.56 μM, respectively. Furthermore, EGFR-IN-62 promotes dose-dependent apoptosis, induces G1/G0 phase arrest, and inhibits cell motility, making it a valuable tool for research in cancer biology and targeted therapies. -
EGFR Inhibitor
EGFR-IN-52 is a potent inhibitor of the epidermal growth factor receptor (EGFR) with IC50 values of 0.358 µM for wild-type EGFR, 86.02 µM for the L858R-TK variant, and 432.67 µM for the T790M-TK resistance mutant. This compound exhibits significant cytotoxicity against various cancer cell lines and is known to induce apoptosis. EGFR-IN-52 is valuable for research applications focusing on targeted cancer therapies and the study of EGFR signaling pathways.
