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Catalog No.
Product Name
Application
Product Information
Citations
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Pan-HER Inhibitor
pan-HER-IN-2 is a reversible, orally active pan-HER inhibitor targeting multiple receptor tyrosine kinases, with IC50 values of 0.72 nM for EGFR, 2.0 nM for HER4, 8.2 nM for EGFRT790M/L858R, and 75.1 nM for HER2. This compound effectively induces apoptosis and exhibits significant antitumor activities. pan-HER-IN-2 is suitable for research applications focused on cancer therapy and the exploration of targeted treatments for HER family receptor-positive tumors. -
EGFR Inhibitor
Gefitinib dihydrochloride is a potent and selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, exhibiting an IC50 of 33 nM. This compound effectively inhibits EGF-stimulated tumor cell proliferation (IC50 of 54 nM) and prevents EGFR autophosphorylation, thereby blocking downstream signaling pathways. Gefitinib dihydrochloride is valuable for cancer research, particularly in the study of lung and breast cancers, due to its ability to induce autophagy and promote apoptosis in tumor cells. -
EGFR Inhibitor
Zorifertinib hydrochloride is a potent orally active inhibitor of the epidermal growth factor receptor (EGFR), demonstrating IC50 values of 0.3 nM, 0.2 nM, and 0.2 nM against wild-type EGFR, EGFR L858R, and EGFR exon 19 deletion variants, respectively. This compound is capable of inducing apoptosis in cancer cells and exhibits significant antitumor activity. Zorifertinib hydrochloride is primarily utilized in research related to non-small cell lung cancer (NSCLC) and hepatocellular carcinoma (HCC). -
JAK2/FLT3 Inhibitor
Flonoltinib sulfate is a potent, orally active dual inhibitor targeting JAK2 and FLT3. It demonstrates significant biological activity with IC50 values of 0.7 nM for JAK2 and 4 nM for FLT3, along with activity against JAK1 and JAK3 at 26 nM and 39 nM, respectively. This compound is primarily utilized in cancer research, particularly in the study of hematological malignancies influenced by aberrant JAK2 and FLT3 signaling pathways. -
JAK1 Inhibitor
Ivarmacitinib sulfate is a selective inhibitor of the Janus kinase 1 (JAK1) pathway, exhibiting a significant preference over JAK2, JAK3, and Tyk2. This compound effectively inhibits JAK1-STAT3 phosphorylation, leading to the apoptosis of hepatic stellate cells. Ivarmacitinib sulfate demonstrates notable anti-proliferative and anti-inflammatory properties, making it a valuable tool for research on hepatic diseases and inflammation-related disorders. -
Aurora/JAK Inhibitor
AT9283 lactic acid is a multi-targeted kinase inhibitor primarily targeting Aurora A/B and JAK2/3. It demonstrates potent biological activity against various cancers, exhibiting IC50 values between 1 to 30 nM for its targets. AT9283 lactic acid effectively inhibits the growth and survival of multiple solid tumors in both in vitro and in vivo models, making it a valuable reagent for cancer research applications. -
c-kit/VEGFR/PDGFR Inhibitor
Famitinib malate is an orally active, multi-targeted kinase inhibitor primarily targeting c-kit, VEGFR-2, and PDGFRβ, with IC50 values of 2.3 nM, 4.7 nM, and 6.6 nM, respectively. This compound induces cell apoptosis and demonstrates significant anti-tumor activity in human gastric cancer cells and xenograft models. Famitinib malate is a valuable tool for research into cancer therapies and mechanisms of action. -
EGFR Inhibitor
SKLB188 is a potent and orally active inhibitor of the epidermal growth factor receptor (EGFR), exhibiting an IC50 of 5 nM. This compound effectively suppresses both MEK/Erk and Akt/mTOR signaling pathways, leading to reduced proliferation of head and neck squamous cell carcinoma (HNSCC) and inducing caspase-dependent apoptosis. SKLB188 is a valuable reagent for research focused on EGFR-overexpressing solid tumors. -
EGFR Inhibitor
EGFR-IN-59 is an epidermal growth factor receptor (EGFR) inhibitor with an IC50 of 190 nM, demonstrating apoptosis-inducing properties. This compound exhibits significant cytotoxicity against non-small cell lung cancer cell lines (A549) with an IC50 of 8.62 µM, while maintaining a lower cytotoxic effect on normal lung fibroblasts (WI38) at 52.6 µM. EGFR-IN-59 is a valuable tool for investigating various cancers, including non-small cell lung cancer (NSCLC), head and neck cancer, breast cancer, and colorectal cancer. -
Pan-HER Inhibitor
pan-HER-IN-1 is an irreversible pan-HER inhibitor that targets multiple human epidermal growth factor receptors (HER) with IC50 values of 0.38 nM for EGFR, 1.6 nM for HER4, 2.2 nM for EGFRT790M/L858R, and 3.5 nM for HER2. This compound effectively induces apoptosis and exhibits significant antitumor activity, making it a valuable tool for cancer research and therapeutic applications aimed at HER-driven malignancies. -
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. -
JAK2/3 Inhibitor
JAK-2/3-IN-3 is a potent inhibitor of JAK2 and JAK3, demonstrating IC50 values of 13.00 nM and 14.86 nM, respectively. It effectively inhibits the autophosphorylation of JAK2 and promotes apoptosis in a dose- and time-dependent manner. This compound is valuable for research into lymphoid malignancies and leukemia, providing insights into the role of JAK signaling pathways in these diseases. -
GLUT1/EGFR Inhibitor
GLUT1/EGFR-IN-1 is a potent inhibitor of both the GLUT1 transporter and the EGFR tyrosine kinase. By targeting the ATP-binding site of EGFR and concurrently inhibiting GLUT1-mediated energy metabolism, GLUT1/EGFR-IN-1 effectively reduces ATP levels, mitochondrial membrane potential, and intracellular lactic acid, while also preventing EGFR nuclear translocation. This compound is applicable in research focusing on nasopharyngeal carcinoma (NPC) and triple-negative breast cancer (TNBC). -
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. -
JAK2 Inhibitor
Fedratinib hydrochloride hydrate is a selective, ATP-competitive inhibitor targeting the JAK2 kinase. With an IC50 of 3 nM for both JAK2 and the mutant JAK2V617F, it demonstrates significant potency. This compound exhibits 35-fold selectivity over JAK1 and 334-fold selectivity over JAK3. Fedratinib hydrochloride hydrate effectively induces apoptosis in cancer cells, making it a valuable tool for research in myeloproliferative disorders. -
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. -
PKD/PIM2 Inhibitor
CRT0066101 is a potent and orally active inhibitor of Protein Kinase D (PKD) with IC50 values of 1 nM, 2.5 nM, and 2 nM for PKD1, PKD2, and PKD3, respectively. Additionally, it serves as an effective PIM2 inhibitor with an IC50 of approximately 135.7 nM. This compound exhibits notable anti-inflammatory activity demonstrated in LPS-induced lung injury models in mice, as well as anticancer effects, making it a valuable tool for research in cancer and inflammation-related studies. -
CK2/PIM1 Inhibitor
CK2/PIM1-IN-1 is a selective inhibitor targeting casein kinase 2 (CK2) and PIM1, demonstrating IC50 values of 3.787 μM and 4.327 μM, respectively. This compound is designed for research into proliferative disorders, particularly cancer, and has potential applications in studying kinase-related conditions such as inflammation, pain, vascular disorders, pathogenic infections, and certain immunological disorders. -
STAT6 Inhibitor
STAT6-IN-7 is a potent inhibitor of STAT6, effectively disrupting the binding of human STAT6 to phosphorylated IL-4 receptor alpha (pIL-4Rα) with an IC50 value of 0.28 μM. Its mechanism of action makes it a valuable tool in the study of inflammatory and allergic diseases, aiding researchers in elucidating the role of STAT6 in these pathological conditions. -
STAT6 Inhibitor
STAT6-IN-9 is a selective inhibitor of Signal Transducer and Activator of Transcription 6 (STAT6), demonstrating an EC50 value of 4 nM. This compound effectively interferes with STAT6 activation driven by the IL-13-IL-13 receptor/IL-4 receptor signaling pathway. Additionally, STAT6-IN-9 inhibits CCL17 secretion with an IC50 of 4.6 nM. It is a valuable tool for investigating chronic inflammatory diseases associated with STAT6 dysregulation, including allergies, asthma, and chronic obstructive pulmonary disease. -
STAT6 Inhibitor
STAT6-IN-10 is a potent inhibitor of signal transducer and activator of transcription 6 (STAT6), exhibiting an EC50 of 0.002 μM. This compound effectively inhibits the secretion of CCL17 in peripheral human whole blood with an IC50 of 0.095 μM, making it a valuable tool for studying inflammatory responses. STAT6-IN-10 is applicable in research focused on dermatological and respiratory conditions, providing insights into therapeutic interventions targeting these pathways. -
STAT6 Inhibitor
STAT6-IN-3 is a potent STAT6 inhibitor designed to selectively target the SH2 domain of STAT6, exhibiting a high binding affinity with an IC50 value of 0.04 μM. This compound is valuable in studying inflammatory processes, particularly in disorders such as asthma, by providing insights into the modulation of STAT6 signaling pathways. Researchers can utilize STAT6-IN-3 to explore its effects on cytokine signaling and immune response regulation. -
STAT3 Inhibitor
SI-109 is a potent inhibitor of the STAT3 SH2 domain, demonstrating an inhibitory constant (Ki) of 9 nM. This compound effectively reduces the transcriptional activity of STAT3 with an IC50 value of 3 μM. SI-109 is utilized in research applications involving antitumor activity and has been instrumental in the development of PROTAC STAT3 degrader SD-36, an important tool in targeted protein degradation studies. -
STAT6 Inhibitor
YM-341619 is a potent STAT6 inhibitor with an IC50 of 0.70 nM, demonstrating effective modulation of Th2 cell differentiation in mouse spleen T cells induced by IL-4, with an IC50 of 0.28 nM. This compound selectively inhibits Th2 differentiation without impacting Th1 cells, making it a valuable tool for research into allergic diseases, including allergic asthma. Its oral bioavailability enhances its utility in in vivo studies aimed at understanding the role of STAT6 signaling in immune responses. -
STAT6 Inhibitor
STAT6-IN-1 is a potent STAT6 inhibitor that specifically targets the SH2 domain of STAT6 with an IC50 value of 0.028 µM. This compound demonstrates significant biological activity in the modulation of signaling pathways associated with allergic lung disease, allergic rhinitis, chronic obstructive pulmonary disease, and various cancer types. STAT6-IN-1 is a valuable tool in research applications focused on elucidating the role of STAT6 in inflammatory and oncogenic processes. -
STAT6 Inhibitor
AS1810722 is a potent inhibitor of STAT6, exhibiting an IC50 of 1.9 nM. This compound possesses a favorable profile regarding CYP3A4 inhibition. As a derivative of fused bicyclic pyrimidine, AS1810722 is poised for research applications in allergic diseases, including asthma and atopic disorders. -
STAT6 Inhibitor
STAT6-IN-4 is a selective inhibitor of Signal Transducer and Activator of Transcription 6 (STAT6), exhibiting an IC50 value of 0.34 μM. This compound has significant potential in the study of inflammatory and allergic conditions, providing researchers the ability to investigate the roles of STAT6 in disease pathogenesis and therapeutic responses. Its application can aid in elucidating the molecular mechanisms underlying STAT6-mediated pathways. -
STAT6 Inhibitor
STAT6-IN-5 is a selective inhibitor of STAT6, demonstrating an IC50 value of 0.24 μM. This compound is primarily utilized in the investigation of inflammatory and allergic diseases, such as atopic dermatitis. Its efficacy in modulating STAT6 activity makes it a valuable tool for exploring therapeutic strategies in related biological pathways. -
STAT6 Inhibitor
STAT6-IN-2 is a selective inhibitor of STAT6, effectively blocking the tyrosine phosphorylation of this transcription factor. By inhibiting STAT6, it reduces the secretion of eotaxin-3, which is pivotal in the inflammatory response. This reagent is particularly valuable for research into immune diseases and allergic inflammatory conditions, including asthma, providing insights into the underlying mechanisms and potential therapeutic targets. -
STAT6 Inhibitor
PM-43I is a potent inhibitor of Signal Transducer and Activator of Transcription 6 (STAT6), effectively reducing its phosphorylation levels. This compound demonstrates significant biological activity in the modulation of immune responses and inflammatory pathways. PM-43I is applicable in research related to allergic lung diseases, allergic rhinitis, chronic obstructive pulmonary disease (COPD), and cancer, making it a valuable tool for investigating STAT6-mediated mechanisms. -
STAT3 Inhibitor
LLL12 is a potent inhibitor of STAT3, specifically targeting its phosphorylation. By interfering with the STAT3 signaling pathway, LLL12 demonstrates significant anti-tumor activity, particularly enhancing the effects of Cisplatin and Paclitaxel on ovarian cancer cell proliferation, migration, and growth. This compound is valuable for research in cancer biology and therapeutic development, especially in exploring combinatorial treatment strategies. -
STAT5a Inhibitor
Stafia-1 is a selective inhibitor of STAT5a, exhibiting a Ki of 10.9 μM and an IC50 of 22.2 μM. It demonstrates significant selectivity for STAT5a over STAT5b and other members of the STAT family. This compound is valuable for research investigating the role of STAT5a in cellular signaling pathways and its implications in various diseases, including cancer and inflammation. -
STAT3 Dimerization Inhibitor
STX-0119 is a selective inhibitor of STAT3 dimerization, targeting the STAT3 signaling pathway. By inhibiting STAT3 transcription with an IC50 of 74 μM, STX-0119 effectively disrupts the aberrant activation of STAT3, which is implicated in various cancers and inflammatory diseases. This compound is valuable for research applications focused on understanding the role of STAT3 in tumorigenesis and potential therapeutic interventions. -
STAT3 Inhibitor
STAT3-IN-25 is a selective inhibitor of Signal Transducer and Activator of Transcription 3 (STAT3). It exhibits significant inhibition of STAT3 luciferase activity in HEK293T cells, displaying an IC50 of 22.3 nM, and inhibits ATP production in BxPC-3 pancreatic cancer cells with an IC50 of 32.5 nM. This compound shows potential for use in research focused on pancreatic cancer and other conditions linked to aberrant STAT3 signaling. -
STAT5b SH2 Inhibitor
Stafib-1 is a selective inhibitor of the STAT5b SH2 domain, exhibiting a Ki value of 44 nM and an IC50 of 154 nM. It effectively disrupts STAT5b signaling, which plays a crucial role in various cellular processes, including proliferation and apoptosis. Stafib-1 is valuable for research applications aimed at understanding oncogenic signaling pathways and exploring potential therapeutic strategies for STAT5b-driven malignancies. -
STAT5b Inhibitor
Stafib-2 is a selective inhibitor of the transcription factor STAT5b, demonstrating an IC50 of 82 nM specifically for STAT5b and 1.7 μM for STAT5a. This compound is critical for studies exploring the role of STAT5b in various biological processes, including cell proliferation and survival. Although Stafib-2 exhibits limited cell permeability, it remains a valuable tool for researchers investigating signaling pathways associated with STAT5b in cancer and other diseases. -
STAT3 Inhibitor
5-FAM-GpYLPQTV-NH2 is a fluorescently labeled peptide that inhibits the signal transducer and activator of transcription 3 (STAT3). This compound exhibits significant biological activity as a STAT3 inhibitor, making it a valuable tool for cancer research. Its fluorescent properties enable easy tracking in various biological assays, facilitating the study of STAT3-mediated pathways in tumor biology. -
STAT5 Inhibitor
HODHBt is a STAT5 inhibitor that disrupts the interaction between STAT5 and SUMO, thereby preventing the SUMOylation of phosphorylated STAT5. This action enhances IL-15 signaling, which significantly improves the cytotoxicity and functionality of natural killer (NK) cells, as well as promotes the generation of cytokine-induced memory-like (CIML) NK cells. HODHBt is valuable for research into HIV infection and cancer therapies. -
STAT6 Inhibitor
PM-81I is a potent inhibitor of STAT6, targeting its SH2 structural domain to effectively reduce STAT6 phosphorylation levels. This compound serves as a valuable tool in research related to allergic lung diseases, allergic rhinitis, chronic obstructive pulmonary disease, and various cancer studies. Its ability to modulate STAT6 activity makes it relevant for elucidating the molecular mechanisms underlying these conditions. -
STAT3 Inhibitor
STAT3-IN-17 is a selective inhibitor of the signal transducer and activator of transcription 3 (STAT3), exhibiting an IC50 of 0.7 μM in HEK-Blue IL-6 assays. This compound demonstrates antiproliferative effects in HeLa cancer cell lines, making it valuable for oncology research. Additionally, STAT3-IN-17 inhibits pyruvate-ferredoxin oxidoreductase (PFOR) and has shown efficacy against Helicobacter pylori, further expanding its potential applications in microbiological studies. -
STAT3 Inhibitor
MM-206 is a potent inhibitor of the STAT3 SH2 domain-phosphopeptide interaction, with an IC50 of 1.2 μM. This compound induces apoptosis in a dose-dependent manner in acute myeloid leukemia (AML) cell lines. MM-206 is valuable for research applications focused on understanding the role of STAT3 in cancer biology and exploring potential therapeutic strategies targeting this pathway. -
STAT3 Inhibitor
STAT3-IN-20 is a selective inhibitor of the STAT3 protein, exhibiting an IC50 value of 0.65 μM. By binding to the SH2 domain, this compound effectively inhibits STAT3 phosphorylation, translocation, and subsequent downstream gene transcription. Demonstrating significant antiproliferative activity, STAT3-IN-20 shows IC50 values of 2.97 μM against STAT3-overactivated DU145 cells and 3.26 μM against MDA-MB-231 cancer cells. Furthermore, STAT3-IN-20 induces cell cycle arrest and apoptosis, making it a valuable tool for research in cancer therapeutics targeting the STAT3 signaling pathway. -
STAT3 Inhibitor
STAT3-IN-14 is a selective inhibitor of Signal Transducer and Activator of Transcription 3 (STAT3), demonstrating potent inhibitory activity against STAT3 phosphorylation. By binding directly to the hinge region of STAT3, this compound effectively disrupts its activity, making it a valuable tool for research applications targeting STAT3-mediated signaling pathways. It is useful in studies of cancer, inflammation, and autoimmune diseases where STAT3 plays a critical role in disease progression. -
CXCR4/STAT3 Inhibitor
Minecoside is a potent inhibitor of the CXCR4 receptor and STAT3 signaling pathway. It demonstrates significant anticancer and anti-inflammatory activities by downregulating CXCR4 expression and suppressing STAT3 activation, which leads to the inhibition of CXCL12-induced cellular invasion. Minecoside has been shown to effectively hinder cancer metastasis and enhance apoptosis, making it a valuable tool for research in cancer biology and therapeutic development. -
STAT3 inhibitor
(+)-Ochromycinone is a natural antibiotic that serves as a potent inhibitor of STAT3. Its primary biological activity is the modulation of signaling pathways involved in cancer progression and inflammatory responses. This compound is widely utilized in research applications focusing on cancer biology and dermatological diseases such as psoriasis. -
STAT3 Inhibitor
Galiellalactone is a selective inhibitor of STAT3 signaling, exhibiting an IC50 value of 250-500 nM. This small, non-toxic, and non-mutagenic fungal metabolite is relevant for research involving castration-resistant prostate cancer, providing insights into the mechanisms of cancer biology and therapeutic resistance. Its specificity towards STAT3 makes it a valuable tool for studying the role of this pathway in various cellular processes. -
STAT3 Inhibitor
MC0704 is a selective STAT3 inhibitor with an IC50 of 2.13 μM. This compound effectively induces apoptosis and triggers cell cycle arrest, demonstrating significant antitumor activity in murine models of breast cancer. MC0704 is a valuable tool for investigating therapeutic strategies in metastatic triple-negative breast cancer (mTNBC) research. -
STAT3 Inhibitor
STAT3-IN-24 is a cell-permeable inhibitor of the Signal Transducer and Activator of Transcription 3 (STAT3). This peptide inhibitor effectively disrupts the recruitment of STAT3 to Janus Kinase 2 (Jak2) and inhibits the phosphorylation of tyrosine 705, thereby preventing STAT3 dimerization and its subsequent nuclear translocation. STAT3-IN-24 is applicable in studies investigating the oncogenic role of STAT3 and its potential as a therapeutic target in various malignancies. -
STAT Inhibitor
JI069 is a selective JAK-STAT inhibitor that effectively targets the STAT signaling pathway. It demonstrates potent inhibition of STAT3, as well as other STAT proteins including STAT1, STAT5, and STAT6, thereby suppressing Th1, Th2, and Th17 differentiation while promoting iTreg differentiation. Due to its ability to inhibit cytokine production from T cells and decrease STAT3 phosphorylation in synovial cells, JI069 exhibits significant therapeutic potential in models of collagen-induced arthritis.
