Catalog No.
Product Name
Application
Product Information
Citations
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VEGFR Inhibitor
CEP-7055 is a selective vascular endothelial growth factor receptor 2 (VEGFR-2) tyrosine kinase inhibitor that demonstrates potent low nanomolar inhibition of human VEGFR-2. This compound shows enhanced selectivity against various tyrosine and serine/threonine kinases, making it a suitable tool for investigating angiogenesis and tumor growth. In vivo studies have confirmed notable antitumor effects across multiple tumor models, and CEP-7055 has advanced into phase I clinical trials as a prodrug designed to improve water solubility and oral bioavailability through its N,N-dimethylglycine ester formulation. -
VEGFR Inhibitor
CPD-002 is a selective inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2), targeting the VEGFR2/PI3K/AKT signaling pathway to inhibit angiogenesis. In addition to its anti-angiogenic properties, CPD-002 demonstrates significant anti-inflammatory activity, making it a valuable tool for research in conditions such as rheumatoid arthritis. This reagent is ideal for investigating the roles of VEGFR2 in various biological processes and therapeutic applications. -
FLuc/VEGFR Inhibitor
GW701427A is a dual inhibitor targeting Fluc and VEGFR2, exhibiting IC50 values of 0.12 μM and 603 nM, respectively. This compound functions as a protein kinase inhibitor, affecting both ATP-dependent and -independent luciferases. GW701427A is valuable for research applications involving Fluc reporter assays and studies on angiogenesis and vascular signaling pathways. -
VEGFR Inhibitor
CEP-5214 is a potent inhibitor of vascular endothelial growth factor receptor 2 (VEGFR-2) tyrosine kinase, derived from an indenopyrrolocarbazole template. With an IC50 value of 8 nM against VEGF-R2, it demonstrates remarkable selectivity over other kinases, exhibiting low-nanomolar inhibition (IC50 of 4 nM). This compound has shown significant antitumor activity in both cellular and in vivo models, and it has advanced to phase I clinical trials in the form of a water-soluble prodrug (CEP-7055) to improve oral bioavailability. Its distinctive mechanism of action makes it valuable for research applications related to cancer and angiogenesis. -
VEGFR Inhibitor
VEGFR-2-IN-20 is a potent inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2). This compound exhibits strong anti-angiogenic activity, making it a valuable tool for investigating mechanisms of tumor growth and metastasis in cancer research. It is particularly useful for studies focused on targeting VEGFR signaling pathways in various malignancies. -
VEGFR-2 Inhibitor
VEGFR-2-IN-26 is a highly potent inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2), demonstrating an IC50 value of 15.5 nM. This compound exhibits significant antiproliferative activity across various cancer cell lines, including leukemic, non-small cell lung, CNS, ovarian, renal, prostate, and breast cancers. VEGFR-2-IN-26 serves as a valuable tool for cancer research, particularly in studies targeting tumor angiogenesis and metastasis. -
TIE-2/VEGFR-2 Inhibitor
TIE-2/VEGFR-2 kinase-IN-3 is a benzimidazole compound that selectively inhibits TIE-2 and VEGFR-2 tyrosine kinase receptors, exhibiting IC50 values of 6.9 nM and 3.5 nM, respectively. This inhibitor is valuable for research focused on angiogenesis, providing insights into tumor growth and vascular development. Its potent activity makes it a significant tool for investigating therapeutic strategies targeting vascular-related diseases. -
TIE-2/VEGFR-2 Inhibitor
TIE-2/VEGFR-2 kinase-IN-4 is a benzimidazole compound that functions as a potent inhibitor of TIE-2 and VEGFR-2 tyrosine kinase receptors, with IC50 values of 5.2 nM and 5.1 nM, respectively. This inhibitor effectively modulates signaling pathways involved in angiogenesis, making it a valuable reagent for research focused on vascular development and tumor growth. Its specificity for both targets allows for detailed studies in cancer biology and therapeutic development. -
PROTAC VEGFR2 Degrader
PROTAC VEGFR-2 Degrader-1 is a targeted protein degradation compound designed to selectively degrade VEGFR-2. It demonstrates minimal VEGFR-2 inhibition with an IC50 exceeding 1 μM, and exhibits limited anti-proliferative activity against EA.hy926 cells, with an IC50 greater than 100 μM. This reagent is valuable for research applications focused on the regulation of VEGFR-2 and its role in vascular biology and related disease mechanisms. -
VEGFR-2/c-Met Inhibitor
VEGFR-2/c-Met-IN-1 is a potent dual inhibitor targeting vascular endothelial growth factor receptor 2 (VEGFR-2) and c-Met, with IC50 values of 138 nM and 74 nM, respectively. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its dual mechanism of action allows for the exploration of therapeutic strategies aimed at inhibiting tumor growth and angiogenesis. -
VEGFR-2 Inhibitor
VEGFR-2-IN-25 is a potent inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR-2), exhibiting an IC50 value of 12.1 nM. This compound is primarily utilized in cancer research to investigate the role of angiogenesis in tumor progression and to evaluate therapeutic strategies targeting the VEGF signaling pathway. Its efficacy makes it a valuable tool for studying anti-tumor effects in various cancer models. -
PROTAC VEGFR2 Degrader
PROTAC VEGFR-2 Degrader-2 primarily targets the vascular endothelial growth factor receptor 2 (VEGFR-2) for degradation through the PROTAC mechanism. This compound displays minimal inhibition of VEGFR-2 activity with an IC50 exceeding 1 μM and demonstrates anti-proliferative effects in EA.hy926 cells, with an IC50 greater than 100 μM. It serves as a valuable tool for studies focused on targeted protein degradation and the modulation of signaling pathways related to angiogenesis. -
VEGFR-2 Inhibitor
VEGFR-2-IN-24 is a potent inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR-2), exhibiting an IC50 value of 0.22 µM. This compound is valuable in tumor research, facilitating the study of angiogenesis and the role of VEGFR-2 in various cancer models. Its efficacy makes it a useful tool for investigating therapeutic strategies targeting tumor vascularization. -
VEGFR-2 Inhibitor
VEGFR-2-IN-65 is a selective inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR-2). It demonstrates high affinity and forms hydrogen bond interactions with Cys180 of the receptor. This compound has been shown to effectively inhibit tube formation in human umbilical vein endothelial cells (HUVECs), making it a valuable tool for investigating angiogenesis and vascular biology pathways. Research applications include the study of tumor angiogenesis and vascular disorders. -
FLuc/VEGFR Inhibitor
GSK248233A is a dual inhibitor targeting FLuc and VEGFR2, exhibiting IC50 values of 1.03 μM and 2 nM, respectively. This compound also demonstrates activity against the AGC family of protein kinases. By inhibiting ATP-dependent and -independent luciferases, GSK248233A holds potential for applications in FLuc reporter assays and related biological research. -
VEGFR Inhibitor
VEGFR-IN-7 is a selective inhibitor of Vascular Endothelial Growth Factor Receptor (VEGFR), primarily involved in regulating angiogenesis. This compound demonstrates potential for modulating angiogenic processes and is particularly relevant in the study of cardiovascular diseases and related pathologies. Its ability to interfere with VEGFR signaling makes it a valuable tool for investigating therapeutic strategies aimed at vascular-related conditions. -
VEGFR Inhibitor
VEGFR/PDGFR-IN-1 is a potent inhibitor of the Vascular Endothelial Growth Factor Receptor (VEGFR) with an IC50 of 0.4 μM. This compound effectively inhibits angiogenesis in Human Umbilical Vein Endothelial Cells (HUVEC), demonstrating potential for application in tumor growth and metastasis research. Its targeted mechanism makes it a valuable tool for studying vascular-related pathologies and developing anti-cancer therapies. -
PDGFR Inhibitor
cis-SU4312 is a potent inhibitor of the Platelet-Derived Growth Factor Receptor (PDGFR) and FLK-1, exhibiting IC50 values of 19.4 μM and 0.8 μM, respectively. Additionally, cis-SU4312 targets several other receptors, including EGFR, HER-2, and IGF-1R with IC50 values of 24.2 μM, 18.5 μM, and 10.0 μM, respectively. Due to its ability to cross the blood-brain barrier, cis-SU4312 is valuable in research applications related to cancer biology and neurobiology. -
SRC/Raf/VEGFR2 Inhibitor
SKLB646 is a multi-target kinase inhibitor with a focus on SRC, Raf, and VEGFR2. It exhibits potent inhibitory activity against SRC and VEGFR2, with IC50 values of 0.002 μmol/L and 0.012 μmol/L, respectively, as well as significant effects on B-Raf and C-Raf. SKLB646 disrupts SRC signaling and inhibits the MAPK pathway by targeting Raf kinases, leading to decreased proliferation, migration, and invasion in human umbilical vein endothelial cells (HUVEC), thereby impeding tumor-induced angiogenesis. It also demonstrates significant anti-proliferative and anti-survival effects on triple-negative breast cancer (TNBC) cell lines, making it a valuable tool for cancer research. -
VEGFR Antagonist
K-106 is a selective vascular endothelial growth factor receptor (VEGFR) antagonist that also inhibits neurotrophic tyrosine kinase receptors (NTRK). This compound exhibits significant biological activity in modulating angiogenesis and neuroprotection, making it a valuable tool for investigating retinal research and related therapeutic applications. Its dual inhibitory profile supports studies focused on vascular and neurological disorders. -
VEGFR Inhibitor
VEGFR-IN-6 is an inhibitor of the vascular endothelial growth factor receptor (VEGFR), known for its ability to impede angiogenesis. This compound is particularly relevant in the study of tumor biology, where angiogenesis plays a critical role in tumor progression and metastasis. VEGFR-IN-6 serves as a valuable tool for researchers investigating the mechanisms of cancer and the development of anti-angiogenic therapies. -
VEGFR2 Kinase Inhibitor
VEGFR2-IN-4 is a selective inhibitor of the VEGFR2 kinase, exhibiting a GI50 value of 0.7 nM. This compound demonstrates significant anti-angiogenic activity, making it a valuable tool for investigating the role of angiogenesis in various biological processes. VEGFR2-IN-4 is suitable for research applications related to rheumatoid arthritis and other angiogenesis-associated conditions. -
PDGFRβ Inhibitor
SU16f is a potent and selective inhibitor of PDGFRβ, exhibiting IC50 values of 10 nM for PDGFRβ, 140 nM for VEGF-R2, and 2.29 μM for FGF-R1. By effectively neutralizing the PDGFRβ receptor, SU16f disrupts the supportive effects of gastric cancer-derived mesenchymal stem cells (GC-MSCs) conditioned medium on gastric cancer cell proliferation and migration. This compound is valuable for research applications focused on gastric cancer and the modulation of tumor microenvironments. -
PDGFR Inhibitor
PDGFR Tyrosine Kinase Inhibitor III is a potent inhibitor of platelet-derived growth factor receptor (PDGFR), along with other kinases such as EGFR, FGFR, PKA, and PKC. This multikinase inhibitor plays a crucial role in modulating various signaling pathways involved in cellular proliferation and survival. Its application extends to the investigation of amyotrophic lateral sclerosis, providing insights into the underlying mechanisms of this neurodegenerative disorder. Researchers can employ this compound to explore therapeutic strategies targeting PDGFR and associated pathways. -
PDGFR Inhibitor
WQ-C-401 is an orally active inhibitor of the platelet-derived growth factor receptor (PDGFR), effectively blocking PDGFR autophosphorylation with EC50 values of 3.5 nM for PDGFRα Y849 and 5.8 nM for PDGFRβ Y1021. This compound significantly inhibits the proliferation and migration of pulmonary artery smooth muscle cells (PASMCs) by interfering with PDGF-BB-induced ERK1/2 phosphorylation, thus reducing collagen I synthesis and enhancing α-smooth muscle actin expression. WQ-C-401 is a valuable tool for studying mechanisms underlying pulmonary vascular remodeling and holds potential for research in pulmonary arterial hypertension. -
PDGFR Antagonist
CT52923 is a selective antagonist of the platelet-derived growth factor receptor (PDGFR) and acts as an ATP-competitive inhibitor. This compound demonstrates significant biological activity relevant to a range of pathological conditions, including atherosclerosis, glomerulonephritis, liver cirrhosis, pulmonary fibrosis, and certain cancers. CT52923 can be utilized to explore therapeutic pathways and mechanisms involved in these diseases. -
PDGFr Inhibitor
PDGFR-IN-2 is a 4-phenoxyquinoline derivative that acts as a selective inhibitor of the platelet-derived growth factor receptor (PDGFr) with an IC50 value of 0.20 μM. By targeting PDGFr tyrosine kinase activity, PDGFR-IN-2 effectively disrupts downstream signaling pathways associated with cell proliferation and migration. This compound is valuable for research applications investigating the role of PDGFr in various pathological conditions, including cancer and fibrotic diseases. -
PDGFR Inhibitor
DMPQ dihydrochloride is a selective inhibitor of human platelet-derived growth factor receptor β (PDGFRβ), exhibiting an IC50 of 80 nM. This compound demonstrates significant potential in research applications focused on PDGFRβ-mediated signaling pathways, which are implicated in a variety of pathological conditions, including cancer and fibrosis. Its potency and selectivity make DMPQ dihydrochloride a valuable tool for investigating the role of PDGFRβ in cellular processes and therapeutic interventions. -
PDGFR Inhibitor
AG 370 is a selective inhibitor of the platelet-derived growth factor receptor (PDGFR), exhibiting potent activity against PDGF-induced mitogenesis with an IC50 of 20 μM. Additionally, AG 370 demonstrates weak inhibitory effects on the epidermal growth factor receptor (EGFR). This compound is valuable for research applications focused on signaling pathways related to cell proliferation and cancer biology. -
PDGFR-α Inhibitor
PDGFRα kinase-IN-2 is a potent inhibitor of the platelet-derived growth factor receptor alpha (PDGFR-α) with an IC50 of 2.1 nM. This compound exhibits significant anticancer activity against HT-29 human colon cancer cells, with an IC50 of 1.48 μM. Additionally, PDGFRα kinase-IN-2 demonstrates anti-angiogenic properties in zebrafish models while exhibiting low embryonic lethality. It is a valuable tool for research focused on colon cancer and the mechanisms of anti-angiogenesis. -
TGFβRI/PDGFRα Inhibitor
BI-4659 is a dual inhibitor of TGFβRI and PDGFRα, exhibiting IC50 values of 19 nM and 99 nM, respectively. This compound effectively inhibits the kinase activities of both receptors, thereby blocking downstream TGFβRI signaling and reducing Smad2/3 phosphorylation without impacting TGF-β1 expression. BI-4659 is suitable for research applications in pulmonary fibrosis, cancer, and renal ischemia-reperfusion injury studies. -
PDGFR Fragment
PDGFR Y1021 peptide (non-phosphorylation) is a specific non-phosphorylated fragment of the platelet-derived growth factor receptor (PDGFR). This peptide effectively inhibits the association of PLCγ with PDGFR via the PLCγ SH2 domain, thereby blocking the mitogenic response. It serves as a valuable tool in research focused on signaling pathways involving PDGFR and its role in cell growth and proliferation. -
PDGFRA Inhibitor
GSK190937 is a type II inhibitor of the platelet-derived growth factor receptor alpha (PDGFRA), exhibiting notable antimalarial activity. This compound effectively inhibits hemozoin formation in malaria parasites, leading to the accumulation of free hemoglobin. GSK190937 demonstrates IC50 values of 0.22 μM, 0.59 μM, and 0.25 μM against Plasmodium falciparum strains NF54, K1, and Dd2, respectively. Additionally, it has an IC50 of 25 μM for CHO cells, making it a valuable tool for malaria research. -
PDGFR Fragment
PDGFR Y1021 peptide (phosphorylation) is a phosphorylated fragment of the platelet-derived growth factor receptor (PDGFR) that facilitates the binding of phospholipase C-gamma (PLCγ) through its SH2 domains. This interaction enhances the production of inositol phosphates and stimulates mitogenic responses. The peptide serves as a valuable tool for research investigating PDGFR signaling pathways and their roles in cellular proliferation and differentiation. -
PDGFR Inhibitor
KN1022 is a selective inhibitor of the phosphorylation of platelet-derived growth factor receptor (PDGFR), with an IC50 value of 0.24 μM. This compound effectively modulates PDGFR signaling pathways, making it a valuable tool for investigating the role of PDGFR in various cellular processes. It is particularly relevant for research in cancer biology, fibrosis, and other diseases associated with abnormal PDGFR activity. -
PDGFR Inhibitor
Sch 13835 is a selective inhibitor of the platelet-derived growth factor receptor (PDGFR), which plays a critical role in cellular processes such as proliferation, differentiation, and survival. This compound exhibits significant inhibitory activity against PDGFR, making it a valuable tool for studying pathways involved in cancer and fibrosis. Its applications include investigating the role of PDGFR in tumor growth and exploring therapeutic strategies for conditions driven by aberrant PDGFR signaling. -
PDGFR-βInhibitor
Tyrphostin AG1433 hydrochloride is a specific and potent inhibitor of PDGFR-β, with additional activity against KDR/Flk-1. It functions as an angiogenesis inhibitor, making it valuable for research into vascular biology and related pathologies. This compound is suitable for studies focused on cancer, fibrosis, and other diseases where angiogenesis plays a critical role. -
P38-α/Syk Inhibitor
TOP1362 is a potent inhibitor targeting P38-α and Syk kinases, with Kd values of 26 nM and 18 nM, respectively. The compound demonstrates an IC50 of 14 nM in Src kinase activity assays, showcasing its efficacy in inhibiting P38-α, Src, and Syk. TOP1362 is applicable in research focused on dry eye syndrome and related pathways. -
Syk Inhibitor
TAS05567 is a highly selective, ATP-competitive inhibitor of Syk, exhibiting an IC50 of 0.37 nM. This compound demonstrates potent inhibition of Syk alongside four other kinases (FLT3, JAK2, KDR, and RET) at IC50 values of 10 nM, 4.8 nM, 600 nM, and 29 nM, respectively. TAS05567 is suitable for research applications related to humoral immune-mediated inflammatory conditions, including various autoimmune and allergic diseases. -
FAK Activator
ZINC40099027 is a selective FAK (Focal Adhesion Kinase) activator that promotes the phosphorylation of FAK while maintaining specificity by not activating its paralogs Pyk2 and Src. This compound enhances wound closure in human intestinal epithelial monolayers and facilitates the healing of ulcers in mouse models through FAK activation. ZINC40099027 is valuable for research focused on gastrointestinal mucosal injury and associated disease mechanisms. -
Src-FAK-Paxillin Inhibitor
JP-153 is a Src-FAK-Paxillin signaling inhibitor that specifically targets the Src-dependent phosphorylation of paxillin at tyrosine 118, leading to downstream inhibition of Akt activation at serine 473. This compound effectively reduces VEGF-induced migration and proliferation in retinal endothelial cells, making it a valuable tool for studying neovascular eye diseases. Researchers can utilize JP-153 to explore the molecular mechanisms underlying angiogenesis and potential therapeutic interventions. -
FAK inhibitor
FAK-IN-14 is a potent inhibitor of focal adhesion kinase (FAK) with an IC50 value of 0.2438 nM. This compound has been shown to induce early apoptosis in U87-MG cells and effectively arrest the cell cycle at the G2/M phase. It is suitable for studies investigating the role of FAK in cancer biology and therapeutic applications targeting cell proliferation and survival. -
FAK1 Inhibitor
Y11 is a selective inhibitor of Focal Adhesion Kinase 1 (FAK1), primarily targeting its autophosphorylation at tyrosine 397. This inhibition leads to reduced phosphorylation activity, which is associated with suppressed tumor growth. Y11 is utilized in research applications focused on cancer biology and the investigation of signaling pathways involved in cell proliferation and metastasis. -
MAPK/FAK Activator
Adhesamine diTFA is a structural molecule that activates the MAPK/FAK signaling pathway. This compound enhances cell adhesion and proliferation in mammalian cell cultures, facilitates the differentiation of primary mouse hippocampal neurons, and promotes their survival. It serves as a valuable tool for research exploring cell signaling mechanisms, neuronal development, and tissue engineering applications. -
MAPK/FAK Activator
Adhesamine is a MAPK/FAK pathway activator that promotes cellular adhesion and proliferation in mammalian cells. It is particularly effective in accelerating the differentiation and enhancing the survival of hippocampal neurons derived from mice in primary culture. This compound is valuable for studies focused on cell adhesion mechanisms, neuronal development, and neuroprotection. -
FAK Inhibitor
FAK-IN-19 is a selective inhibitor of Focal Adhesion Kinase (FAK) that has been characterized through co-crystal structure analysis with the protein. This compound exhibits significant anticancer properties, making it a valuable reagent for research applications aimed at understanding FAK's role in tumor biology and cancer progression. It is particularly relevant for studies focusing on cell adhesion, migration, and metastasis. -
FAK Inhibitor
FAK Inhibitor 2 is a highly effective focal adhesion kinase (FAK) inhibitor, exhibiting an IC50 of 0.07 nM. This compound demonstrates significant antitumor and anti-angiogenesis activities, making it a valuable tool for cancer research. It can be utilized to investigate the role of FAK in tumor progression and vascular development, providing insights into potential therapeutic strategies. -
FAK Inhibitor
FAK-IN-1 is a selective inhibitor of focal adhesion kinase (FAK), a critical regulator of cell adhesion and signaling. This compound exhibits potent antitumor activity, making it a valuable tool for cancer research. Its inhibitory action on FAK can disrupt tumor cell migration and survival, providing insights into cancer metastasis and potential therapeutic strategies. -
Fak Ligand
Defactinib analogue-1 is a ligand that targets focal adhesion kinase (FAK), facilitating the development of proteolysis-targeting chimeras (PROTACs) like FAK degrader 1. This compound is essential for research applications focused on FAK modulation and its role in cellular signaling pathways related to cancer progression and metastasis. Its utility in synthesizing targeted protein degraders makes it a valuable tool for investigating FAK-associated biological processes.
