Catalog No.
Product Name
Application
Product Information
Citations
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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. -
EGFRvIII Epitope
EGFRvIII peptide is a synthetic epitope derived from the EGFRvIII variant, specifically designed to bind to MHC I molecules. This peptide is known to induce apoptosis and elicit targeted immune responses against glioblastoma, particularly when used in conjunction with Flagellin B. It is a valuable tool for research in cancer immunotherapy and the development of personalized medicine approaches for glioblastoma treatment. -
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. -
EGFR Inhibitor
EGFR-IN-3 is a selective inhibitor of the epidermal growth factor receptor (EGFR), demonstrating an IC50 of 0.32 µM against EGFR wild-type kinase. This compound exhibits significant cytotoxic effects on various cancer cell lines and promotes apoptosis, making it a valuable tool for studies related to cancer biology and therapeutic development targeting EGFR signaling pathways. -
EGFRT790M/L858R Inhibitor
EGFR T790M/L858R-IN-2 is a selective inhibitor of the EGFR T790M and L858R mutants, exhibiting IC50 values of 3.5 nM and 1290 nM for these targets, respectively. This compound effectively reduces the phosphorylation of EGFR, AKT, and ERK1/2, subsequently inducing apoptosis and causing cell cycle arrest in the G1 phase. EGFR T790M/L858R-IN-2 demonstrates significant anti-cancer activity, making it a valuable tool for research in targeted therapies for lung cancer and other malignancies associated with these mutations. -
EGFR-TKI
TAS-121 is a selective, covalent third-generation mutant EGFR-tyrosine kinase inhibitor (EGFR-TKI) that targets various EGFR mutations, including L858R (IC50=1.7 nM), Ex19del (IC50=2.7 nM), L858R/T790M (IC50=0.56 nM), and Ex19del/T790M (IC50=1.1 nM), as well as wild-type EGFR (IC50=8.2 nM). It also exhibits inhibitory activity against HER2 and HER4 with IC50s of 110 and 2.6 nM, respectively. TAS-121 effectively inhibits EGFR phosphorylation and downstream signaling pathways, leading to reduced cell proliferation and induction of apoptosis. Its antitumor efficacy has been demonstrated in xenograft models utilizing SW48 (EGFR G719S) and NCI-H1975 (EGFR L858R/T790M) cell lines. -
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. -
EGFR Inhibitor
EGFR-IN-117 is a potent EGFR inhibitor designed to target mutated forms of the epidermal growth factor receptor. It exhibits significant inhibitory activity against a range of EGFR mutant cell lines, including H1975, PC-9, BaF3-EGFRL858R/T790M/C797S, and BaF3–C797S/Del19/T790M, with IC50 values of 13 nM, 19 nM, 1.2 nM, and 1.3 nM, respectively. In addition to its antiproliferative effects, EGFR-IN-117 induces apoptosis and demonstrates antitumor efficacy in preclinical mouse models, making it a valuable tool for cancer research. -
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. -
FLT3/JAK2 Inhibitor
JAK2/FLT3-IN-3 is a potent dual inhibitor of FLT3 and JAK2, exhibiting IC50 values of 2.01 nM for JAK2, 0.51 nM for FLT3, and 104.40 nM for JAK3. This compound induces apoptosis in cancer cells and demonstrates significant antitumor activity. Its ability to inhibit both FLT3 and JAK2 pathways makes it a valuable tool for research related to hematological malignancies and targeted cancer therapies. -
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. -
EGFR Inhibitor
EGFR-IN-161 is a potent and reversible inhibitor targeting L858R/T790M/C797S mutant EGFR kinases, demonstrating an IC50 of 0.87 nM. This compound effectively induces apoptosis, causes G1-phase cell cycle arrest, and inhibits migration in tumor cells, making it a valuable tool for cancer research focused on EGFR mutations. Its specificity and efficacy provide significant potential in the study of targeted therapies for resistant forms of non-small cell lung cancer. -
EGFR Inhibitor
EGFR Kinase Inhibitor 1 is a selective inhibitor targeting the epidermal growth factor receptor (EGFR), exhibiting IC50 values of 37 nM for wild-type, 1.7 nM for L858R/T790M, and greater than 300 nM for L858R/T790M/C797S mutant variants. This compound induces apoptosis and promotes cell cycle arrest at the G0/G1 phase, effectively inhibiting cell motility. Its strong antiproliferative and anti-tumor activities make it a valuable tool for research in cancer biology, particularly in studies related to EGFR-driven malignancies. -
EGFR Inhibitor
EGFR-IN-56 is a potent inhibitor of the epidermal growth factor receptor (EGFR), demonstrating IC50 values of 541.7 nM and 132.1 nM against the EGFRT790M and EGFRT790M/L858R mutations, respectively. This compound significantly disrupts cell cycle progression by blocking cancer cells in the G2/M phase and facilitating late apoptosis. It is suitable for studies examining the therapeutic potential of EGFR inhibition in cancer research. -
EGFR Inhibitor
EGFR-IN-57 is a potent EGFR tyrosine kinase inhibitor with an IC50 of 0.054 µM, demonstrating significant inhibitory activity against additional targets including VEGFR-2, CK2α, topoisomerase IIβ, and tubulin polymerization, with respective IC50 values of 0.087, 0.171, 0.130, and 3.61 µM. This compound effectively induces cell cycle arrest at the G2/M and pre-G1 phases, promoting apoptosis in cancer cells. EGFR-IN-57 is utilized in research applications focused on cancer therapy, specifically targeting EGFR signaling pathways and elucidating mechanisms of tumor growth and resistance. -
EGFR Inhibitor
EGFR/microtubule-IN-1 is a dual inhibitor targeting epidermal growth factor receptor (EGFR) and tubulin. It exhibits an IC50 of 10.66 nM for EGFR inhibition, effectively reducing phosphorylation levels of EGFR, AKT, and ERK. Additionally, this compound disrupts tubulin polymerization and induces apoptosis, making it a valuable tool for cancer research and studies focused on cell signaling pathways and microtubule dynamics. -
JAK3-Inhibitor
JAK3 covalent inhibitor-2 is a selective covalent inhibitor targeting Janus kinase 3 (JAK3), exhibiting an IC50 of 7.2 nM. This compound demonstrates anti-inflammatory activity, low toxicity, and favorable bioavailability, making it suitable for research applications involving autoimmune diseases and inflammatory disorders. Its specificity for JAK3 supports investigations into therapeutic strategies aimed at modulating immune responses. -
EGFR Inhibitor
EGFR-IN-152 is a highly selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, demonstrating significant inhibitory activity against the EGFR L858R/T790M/C797S mutant isoforms, with an IC50 of 40 nM. This compound effectively induces G0/G1 phase cell cycle arrest and apoptosis, leading to the inhibition of colony formation and cell proliferation in non-small cell lung cancer (NSCLC) models. EGFR-IN-152 serves as a valuable tool for research focusing on NSCLC and novel therapeutic strategies targeting EGFR mutations. -
EGFR Inhibitor
EGFR-IN-97 is a selective inhibitor of the epidermal growth factor receptor (EGFR). This compound demonstrates potent inhibitory activity against Ba/F3 cells expressing EGFR mutations, specifically L858R/T790M/C797S and Del19/T790M/C797S, with IC50 values of 0.42 μM and 0.41 μM, respectively. Additionally, EGFR-IN-97 effectively induces apoptosis in NCI-H1975 cells harboring the EGFR L858R/T790M/C797S mutations at a concentration of 0.8 μM. This reagent is valuable for research focused on targeted therapies in EGFR-mutant cancers. -
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. -
EGFR/HER2 Inhibitor
EGFR/HER2-IN-6 is a potent inhibitor of EGFR and HER2 kinases, as well as dihydrofolate reductase (DHFR), with IC50 values of 0.122 μM, 0.078 μM, and 0.585 μM, respectively. This compound displays significant anticancer activity across various cancer cell lines, demonstrating a favorable safety profile and selectivity. EGFR/HER2-IN-6 is valuable for research on cancer therapeutics targeting these critical pathways. -
EGFR/BRAFV600E Inhibitor
EGFR/BRAFV600E-IN-1 is a potent dual inhibitor targeting EGFR and the BRAFV600E mutation, with IC50 values of 0.08 µM and 0.15 µM, respectively. This compound effectively induces apoptosis and induces cell cycle arrest in the pre-G1 and G2/M phases. Additionally, it demonstrates significant antiproliferative activity against A-549, MCF-7, Panc-1, and HT-29 cell lines, with IC50 values of 1.2 µM, 0.79 µM, 1.3 µM, and 1.23 µM, respectively, making it valuable for cancer research focused on these targets. -
EGFR Inhibitor
EGFR-IN-88 is a selective epidermal growth factor receptor (EGFR) inhibitor with an IC50 of 87 nM. The compound demonstrates cytotoxic effects on A549 cells, exhibiting an IC50 of 3.902 μM, and induces apoptosis in these cells. This compound is valuable for research focused on cancer therapies that target EGFR signaling pathways. -
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. -
EGFR Inhibitor
EGFR-IN-26 is a selective inhibitor of the epidermal growth factor receptor (EGFR), derived from patent WO2019162323A1, compound I-028. This compound significantly impedes EGFR activity, making it a valuable tool for investigating its role in cancer biology. It is applicable in cancer research, particularly in studies focused on targeting EGFR signaling pathways to develop novel therapeutic strategies.
