Catalog No.
Product Name
Application
Product Information
Citations
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EML4-ALK PROTAC Degrader
Pro-PEG3-BA is a targeted PROTAC degrader that specifically degrades EML4-ALK and EGFR mutants, with DC50 values of 0.42 μM and 13.50 μM, respectively. It effectively inhibits proliferation and induces cell cycle arrest and apoptosis in non-small cell lung cancer (NSCLC) cell lines in vitro. In vivo studies reveal that Pro-PEG3-BA rewires the ubiquitin-proteasome system, leading to a reduction in EML4-ALK protein levels while demonstrating a favorable safety profile. This reagent is suitable for research focused on non-small cell lung cancer treatments. -
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. -
IGF-1R Inhibitor
KW-2450 tosylate is a selective inhibitor of the insulin-like growth factor-1 receptor (IGF-1R), as well as Aurora A and B kinases. It effectively induces apoptosis in cancer cells, demonstrating significant anticancer activity, particularly against triple-negative breast cancer. This compound is valuable for research applications involving cancer biology and therapeutic targeting of kinase signaling pathways. -
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. -
FLT3 Inhibitors
FLT3-IN-32 is a highly selective, orally bioavailable inhibitor of the FLT3 receptor tyrosine kinase. It effectively targets FLT3-activating mutations, promoting apoptosis in malignant cells. In vivo studies demonstrate significant anti-tumor efficacy in MV4-11 xenograft models within NOD/SCID mice, leading to notable extensions in survival. FLT3-IN-32 is valuable for research applications focused on acute myeloid leukemia. -
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. -
VEGFR-2 Inhibitor
VEGFR-2-IN-23 is a highly selective inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR-2), exhibiting an IC50 value of 0.34 nM. This compound demonstrates significant antitumor activity by inducing apoptosis and causing cell cycle arrest at the G1 phase. VEGFR-2-IN-23 is particularly relevant for research focused on oncology and angiogenesis, providing valuable insights into therapeutic strategies targeting vascular growth pathways. -
TRK Inhibitor
TRK-IN-32 is a potent inhibitor of TRK proteins, effectively targeting TRKWT, TRKG595R, and TRKG667C with IC50 values of 0.08 nM, 2.14 nM, and 0.68 nM, respectively. This compound exhibits significant antiproliferative activity against Ba/F3 cell lines expressing various TRK fusion proteins, including wild type and mutant forms. TRK-IN-32 also induces apoptosis in Ba/F3-TRKAWT and Ba/F3-TRKAG667C cells, making it a valuable tool for investigating the role of TRK signaling in a range of cancers, including thyroid cancer and secretory breast carcinoma. -
c-Met Kinase Inhibitor
c-Met-IN-10 is a highly potent inhibitor of the c-Met kinase, exhibiting an IC50 value of 16 nM. This compound demonstrates significant inhibitory activity against various cancer cell lines, including A549, H460, and HT-29, with IC50 values ranging from 0.56 to 1.59 μM. c-Met-IN-10 effectively suppresses colony formation in HT-29 cells, induces apoptosis in HT-29 and A549 cells, and inhibits A549 cell motility. This reagent is valuable for research applications focused on cancer biology and therapeutic interventions targeting c-Met pathways. -
FLT3 Inhibitor
HSB401 is an orally active FLT3 inhibitor with IC50 values of 28, 5, 72, and 51 nM for FLT3-WT, FLT3-D835Y, FLT3-ITD-F691L, and FLT3-ITD, respectively. It effectively downregulates FLT3 signaling, leading to cell cycle arrest and apoptosis in sensitive cells. Notably, HSB401 spares c-KIT inhibition, minimizing the risk of myelosuppression. This compound has demonstrated significant tumor growth suppression in the MV4-11 xenograft mouse model and is valuable for research in acute myeloid leukemia. -
PROTAC IRAK4 Degrader
KT-474 hydrochloride is a potent PROTAC degrader targeting IRAK4, exhibiting significant anti-tumor properties. This compound inhibits the cell cycle and induces apoptosis in affected cells, demonstrating tumor regression in xenograft models of MYD88-mutated ABC DLBCL. Additionally, KT-474 features an alkyne group facilitating click chemistry, allowing for copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, making it a valuable tool for chemical biology research. -
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. -
c-Met Inhibitor
c-Met-IN-14 is a selective inhibitor of the c-Met kinase, classified as an N-sulfonylamidine derivative, with an IC50 value of 2.89 nM. This compound effectively inhibits c-Met phosphorylation, leading to the arrest of the cell cycle at the G2/M phase and demonstrating significant anticancer activity. Additionally, c-Met-IN-14 induces apoptosis in A549 lung cancer cells in a dose-dependent manner, making it a valuable tool for cancer research and therapeutic studies targeting c-Met signaling pathways. -
TRK Inhibitor
TRK-IN-23 is a selective TRK inhibitor demonstrating potent biological activity with IC50 values of 0.5 nM, 9 nM, 14 nM, 4.4 nM, and 4.8 nM against TRKA, TRKC, TRKAG595R, TRKAF589L, and TRKAG667C, respectively. This compound effectively induces apoptosis in Ba/F3 cells expressing TRKAG595R and TRKAG667C. TRK-IN-23 is valuable for researchers investigating TRK signaling pathways and potential therapeutic interventions in TRK-driven malignancies. -
FLT3 Inhibitor
SILA-123 is a potent FLT3 inhibitor, demonstrating IC50 values of 2.1 nM for FLT3-WT and 1.0 nM for FLT3-ITD. This compound effectively inhibits FLT3 phosphorylation and disrupts downstream signaling pathways, resulting in apoptosis through cell cycle arrest in the G0/G1 phase. SILA-123 is particularly valuable in research related to acute myeloid leukemia. -
VEGFR2 Inhibitor
VEGFR-2-IN-19 is a potent inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR2). This compound has been shown to induce apoptosis in cancer cells and elevate intracellular levels of reactive oxygen species. VEGFR-2-IN-19 is primarily utilized in cancer research, offering potential therapeutic insights into tumor progression and vascularization. -
FLT3 Inhibitor
JH-IX-179 is a potent FLT3 inhibitor with an IC50 of 4 nM for FLT3-ITD and 10 nM for FLT3-D835Y variants. This compound effectively induces cell cycle arrest in the G1 phase and promotes apoptosis in cells expressing the FLT3-ITD mutation. JH-IX-179 is primarily utilized in research focused on acute myeloid leukemia (AML), providing valuable insights into therapeutic strategies targeting FLT3 signaling pathways. -
CSF-1R Inhibitor
CSF1R-IN-22 is a selective inhibitor of the colony-stimulating factor 1 receptor (CSF-1R) with an IC50 value of less than 6 nM. This compound enhances CXCL9 secretion from M2 macrophages and promotes CD8+ T cell infiltration, thereby amplifying anti-tumor immune responses, particularly in combination with anti-PD-1 therapies. CSF1R-IN-22 effectively reprograms M2-like tumor-associated macrophages (TAMs) to the M1 phenotype, reshaping the tumor microenvironment by increasing CD8+ T cell recruitment and decreasing immunosuppressive regulatory T cells and myeloid-derived suppressor cells (MDSCs). -
FLT3/HDAC Inhibitor
HDAC-IN-63 is a dual inhibitor targeting both FLT3 and HDAC, with IC50 values of 0.844 nM for FLT3 and 30.0 nM for HDAC1. It demonstrates potent inhibition of MV4-11 cell proliferation, with an IC50 of 92 nM, and effectively induces apoptosis while arresting the cell cycle in MV4-11 cells. This compound serves as a valuable research tool for the study of acute myeloid leukemia (AML) and the exploration of novel therapeutic strategies. -
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. -
VEGFR-2 Inhibitor
VEGFR-2-IN-13 is a potent inhibitor of the vascular endothelial growth factor receptor-2 (VEGFR-2), demonstrating an IC50 value of 3.4 nM. This compound effectively disrupts the cell cycle in HepG2 cells by inducing G2/M phase arrest and triggering apoptosis. VEGFR-2-IN-13 is valuable for research applications focusing on angiogenesis, cancer development, and therapeutic interventions targeting tumor growth. -
VEGFR-2 Inhibitor
VEGFR-2-IN-28 is a selective inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR-2) with an IC50 value of 0.83 µM. This compound has been shown to induce apoptosis in cancer cells, highlighting its potential as an anticancer agent. VEGFR-2-IN-28 is suitable for research applications focused on tumor vascularization and the mechanisms of cancer cell survival signaling. -
FLT3 Inhibitor
FLT3-IN-31 is a potent inhibitor of FLT3, exhibiting IC50 values of 0.16 nM for the wild-type FLT3 receptor and 2.4 nM for the FLT3-D835Y mutant. It demonstrates significant antiproliferative activity by decreasing the protein expression of phosphorylated FLT3, STAT5, and ERK. Additionally, FLT3-IN-31 induces apoptosis and triggers cell cycle arrest at the G1 phase, making it a valuable tool for research in targeted cancer therapies and leukemia treatment. -
FLT3/HDAC Inhibitor
FLT3/HDAC-IN-3 is a dual inhibitor targeting FLT3 and HDAC, with a potent inhibitory effect on FLT3 (IC50 = 14 nM) and HDAC isoforms, including HDAC1 (IC50 = 27 nM) and HDAC6 (IC50 = 20 nM). This compound demonstrates selective inhibition, exhibiting reduced activity against HDAC8 and no activity toward HDAC4. FLT3/HDAC-IN-3 has shown anti-proliferative effects across various hematological malignancy cell lines and demonstrates efficacy in the Jeko-1 xenograft model without significant toxicity. It is suitable for research focused on hematological malignancies and the role of dual inhibition in therapeutic strategies. -
SRC Inhibitor
SI-2 is a selective inhibitor of steroid receptor coactivator-3 (SRC-3), effectively reducing both its transcriptional activity and protein levels in cells. This compound exhibits significant cytotoxicity against cancer cells and inhibits the migration of MDA-MB-468 breast cancer cells, promoting apoptosis in these cells. In vivo studies demonstrate that SI-2 suppresses tumor growth in mouse models while showing minimal toxicity to the heart and other vital organs at a dosage of 20 mg/kg. -
PROTAC c-Met Degrader
PROTAC c-Met Degrader-4 is a potent orally active PROTAC designed to target c-MET for degradation. It exhibits remarkable intracellular degradation potency with a DC50 value of less than 0.5 nM and effectively induces cell cycle arrest and apoptosis while inhibiting cell invasion and migration. This compound is particularly useful in cancer research, demonstrating the ability to suppress proliferation and inhibit the growth of various cancers, including non-small cell lung cancer and gastric cancer. In vivo studies also highlight its effectiveness in reducing tumor growth in Hs746T xenograft models. -
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. -
ALK Inhibitor
KF-20444 is a selective ALK inhibitor that effectively penetrates the blood-brain barrier. It demonstrates potent activity against ALK fusion proteins such as EML4-ALK and various ALK resistance mutations, including L1196M, G1202R, and F1174L. By inhibiting ALK phosphorylation in ALK-driven cancer cell lines, KF-20444 suppresses cell proliferation and promotes apoptosis. This compound shows significant anti-tumor efficacy in mouse models of ALK-positive non-small cell lung cancer (NSCLC) and neuroblastoma, making it a valuable tool for research on ALK-driven malignancies. -
FGFR2 Kinase Inhibitor
Picrasidine Q is a FGFR2 kinase inhibitor derived from the alkaloid components of Angelica keiskei. It exhibits significant anti-cancer properties by inducing apoptosis and causing G1 phase cell cycle arrest in human esophageal cancer cell lines. This compound is valuable for research focused on cancer biology and the molecular mechanisms underlying cell transformation and proliferation. -
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. -
VEGFR-2/β-tubulin Inhibitor
VEGFR-2-IN-22 is a dual inhibitor targeting VEGFR-2 and β-tubulin polymerization, demonstrating an IC50 of 19.82 nM against VEGFR-2. This compound promotes apoptosis, making it a valuable tool for studying angiogenesis and cancer biology. Its mechanism of action provides insights into vascular endothelial growth factor pathways and their role in tumor progression. -
FLT3 Inhibitor
Tuspetinib dihydrochloride is a selective FLT3 inhibitor that demonstrates potent inhibitory activity with IC50 values of 1.1 nM for FLT3 WT, 1.8 nM for FLT3 ITD, and 1.0 nM for FLT3 D835Y kinases. As a reversible type I inhibitor, it effectively modulates downstream signaling pathways, including p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib dihydrochloride is utilized in research for its ability to inhibit proliferation and induce apoptosis in leukemic cells, making it significant for studies on hematological malignancies. -
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. -
FLT3/MNK2 Inhibitor
K783-0308 is a potent and selective dual inhibitor of FLT3 and MNK2, demonstrating IC50 values of 680 nM and 406 nM, respectively. This compound effectively inhibits the growth of acute myeloid leukemia (AML) cell lines, MOLM-13 and MV-4-11, with IC50 values of 10.5 µM and 10.4 µM. Additionally, K783-0308 promotes apoptosis and induces cell cycle arrest in the G0/G1 phase, making it a valuable tool for research into AML and related pathways. -
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. -
FLT3-ITD Inhibitor
FLT3-ITD-IN-3 is a potent inhibitor of FLT3-ITD (FLT3 internal tandem duplication), primarily targeting the FLT3 signaling pathway. This compound effectively disrupts FLT3 signal transduction, leading to G0/G1 cell cycle arrest and the induction of apoptosis in malignant cells. FLT3-ITD-IN-3 is valuable for research applications focused on acute myeloid leukemia (AML) and related hematological disorders. -
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. -
PARP1/c-Met Inhibitor
PARP1/c-Met-IN-1 is a selective dual inhibitor targeting PARP1 and c-Met, demonstrating IC50 values of 3.3 nM and 32.2 nM, respectively. This compound effectively induces apoptosis and causes cell cycle arrest in the G2/M phase in MDA-MB-231 cells. Additionally, PARP1/c-Met-IN-1 has shown significant antitumor activity in murine models, making it a valuable tool for cancer research and therapeutic development. -
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. -
FLT3 Inhibitor
FLT3-IN-33 is a potent FLT3 inhibitor with an IC50 value of 7.82 nM, demonstrating significant anti-cancer activities, particularly against acute myeloid leukemia (AML) cell lines such as MV4-11 and MOLM-13. This compound effectively induces apoptosis in cancer cells and inhibits the phosphorylation of FLT3 signaling pathways. FLT3-IN-33 is suitable for research applications targeting AML and other malignancies, providing valuable insights into therapeutic strategies and cellular responses. -
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. -
EGFR/VEGFR2 Inhibitor
EGFR/VEGFR2-IN-3 is a selective inhibitor of the epidermal growth factor receptor (EGFR) and vascular endothelial growth factor receptor 2 (VEGFR-2), demonstrating IC50 values of 0.129 µM and 0.142 µM, respectively. This compound also exhibits activity against cyclooxygenase-2 (COX-2) with an IC50 of 3.428 µM. EGFR/VEGFR2-IN-3 has been shown to induce cytotoxic effects, promoting apoptosis and causing cell cycle arrest at the G2/M phase. Its dual inhibition profile makes it a valuable tool for research in cancer biology and therapeutic development. -
Anti-Inflammatory Agent
2,4′-Dihydroxybenzophenone acts as an anti-inflammatory agent by targeting the hydrophobic pocket of MD2, effectively inhibiting the dimerization of TLR4. This compound demonstrates significant biological activity by suppressing LPS-induced mitochondrial reactive oxygen species (mtROS) production and attenuating the inflammatory response through downregulation of pro-inflammatory mediators, including MyD88, p-IRAK4, and NF-κB. Additionally, 2,4′-Dihydroxybenzophenone serves as an effective UV absorber, enhancing its utility in research on oxidative stress and inflammation.
