Catalog No.
Product Name
Application
Product Information
Citations
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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. -
HIF1-α Inhibitor
Oltipraz metabolite M2 is an active metabolite that serves as a HIF-1α inhibitor. It enhances mitochondrial fuel oxidation and inhibits lipogenesis in the liver by activating AMPK, particularly in high-fat diet-fed mouse models. This compound is valuable for research focused on hepatic steatosis and steatohepatitis. -
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. -
FAK PROTAC degrader
FAK PROTAC B5 is a potent degrader targeting focal adhesion kinase (FAK) with an IC50 of 14.9 nM. This compound exhibits significant FAK degradation capabilities along with antiproliferative effects. Furthermore, it demonstrates notable plasma stability and moderate membrane permeability, effectively inhibiting cell migration and invasion. FAK PROTAC B5 is suitable for research applications focused on cancer biology and cellular signaling pathways. -
FAK Inhibitor
FAK-IN-23 is a selective inhibitor of focal adhesion kinase (FAK), a critical regulator of cell adhesion, migration, and survival. This compound effectively disrupts FAK activity, leading to the modulation of cellular signaling pathways associated with cancer progression and metastasis. FAK-IN-23 is primarily used in cancer research to investigate the role of FAK in tumor biology and to evaluate potential therapeutic strategies targeting FAK-related pathways. -
FAK Inhibitor
PH11 is a potent focal adhesion kinase (FAK) inhibitor that enhances TRAIL-induced apoptosis in TRAIL-resistant PANC-1 cells while sparing normal human fibroblasts. This compound operates by downregulating c-FLIP through the inhibition of FAK and the phosphatidylinositol-3-kinase (PI3K)/AKT signaling pathways, thereby reinstating the TRAIL apoptotic cascade. PH11 represents a promising therapeutic strategy for pancreatic cancer by selectively targeting the c-FLIP regulatory pathway without affecting caspase-8 processing, thus circumventing TRAIL resistance. Ongoing research will further delineate PH11's mechanism of action and its implications in overcoming resistance in TRAIL-based therapies for pancreatic cancer. -
PROTAC FAK Degarder
BSJ-04-146 is a selective PROTAC that targets focal adhesion kinase (FAK) for degradation, exhibiting an IC50 of 26 nM. It demonstrates rapid and robust degradation of FAK in cancer cells while maintaining high specificity across the proteome, and it induces prolonged degradation in murine models. The activity of BSJ-04-146 relies on the ubiquitin-proteasome system, making it a valuable tool for investigating pathways associated with pancreatic cancer and triple-negative breast cancer. -
FAK Inhibitor
FAK-IN-3 is a potent inhibitor of focal adhesion kinase (FAK), a critical regulator of cell adhesion and signaling. This compound effectively reduces migration and invasion in PA-1 ovarian cancer cells while downregulating the expression of matrix metalloproteinases MMP-2 and MMP-9. FAK-IN-3 demonstrates significant tumor growth and metastasis inhibition, making it a valuable tool for research in ovarian cancer and related fields. -
FAK Inhibitor
FAK-IN-26 is a potent inhibitor of Focal Adhesion Kinase (FAK) with an IC50 of 0.87 nM, effectively penetrating the blood-brain barrier. It has been shown to significantly reduce tumor cell viability, inhibit cancer stem cell activity, and diminish cell migration in A549 and SKOV-3 cell lines. In vivo studies demonstrate robust anti-cancer activity, achieving tumor inhibition rates of 59.15% and 57.9% in A549 and SKOV-3 mouse models, respectively, highlighting its potential for cancer research applications. -
FAK Inhibitor
FAK-IN-21 is a selective inhibitor of Focal Adhesion Kinase (FAK) with an IC50 of 37.52 nM. This compound effectively inhibits cell growth and the phosphorylation of FAK, making it a valuable tool in cancer research. FAK-IN-21 is particularly useful for studies related to diffuse gastric cancer, providing insights into the mechanistic role of FAK in tumor progression. -
FAK Ligand
FAK Ligand-5 functions as a FAK ligand, enabling the targeted modulation of focal adhesion kinase. This compound is essential for the synthesis of PROTAC molecules, particularly in the development of FAK degraders such as PROTAC FAK degrader 4. It serves as a valuable tool in cancer research, facilitating investigations into FAK signaling pathways and their implications in tumor progression. -
FAK Inhibitor
Defactinib-d6 is a deuterium-labeled derivative of Defactinib, a potent inhibitor of focal adhesion kinase (FAK). It exhibits antiangiogenic and antineoplastic properties, making it valuable for cancer research. This reagent is suitable for studies investigating FAK-related signaling pathways and their role in tumor growth and metastasis. -
FAK Activator
FAK activator-1 is a selective activator of Focal Adhesion Kinase (FAK) that enhances phosphorylation at Tyr-397, thereby promoting FAK activation. This reagent is particularly effective in advancing mucosal healing processes. FAK activator-1 is applicable in research focused on NSAID-associated gastrointestinal mucosal injury, providing valuable insights into cellular mechanisms involved in tissue repair and integrity. -
FAK Inhibitor
FAK-IN-9 is a potent inhibitor of focal adhesion kinase (FAK) with an IC50 of 27.44 nM. This compound has demonstrated the ability to induce apoptosis in triple-negative breast cancer (TNBC) cells, highlighting its potential as a therapeutic agent in cancer research. FAK-IN-9 can be utilized to explore the role of FAK in cell signaling and its implications in various cancer types. -
FAK Inhibitor
FAK-IN-6 is a potent inhibitor of focal adhesion kinase (FAK), exhibiting an IC50 value of 1.415 nM. This compound demonstrates significant anti-proliferative activity against various cancer cell lines, making it valuable for in vitro studies. FAK-IN-6 is particularly relevant for research focused on pancreatic cancer, providing a tool for elucidating the role of FAK in tumor progression and potential therapeutic strategies. -
FAK Inhibitor
FAK Inhibitor 6 specifically targets focal adhesion kinase (FAK) and is recognized for its potent inhibitory effects, with an IC50 of 28.2 nM. This compound demonstrates reduced cytotoxicity (IC50 = 3.32 µM) while effectively inducing apoptosis in MDA-MB-231 breast cancer cells in a dose-dependent manner. Additionally, FAK Inhibitor 6 effectively halts the cell cycle progression of MDA-MB-231 cells at the G0/G1 phase, making it a valuable tool for research in cancer biology and therapeutic development. -
VEGFR2/FAK Inhibitor
ZINC09875266 is a dual inhibitor that specifically targets Vascular Endothelial Growth Factor Receptor 2 (VEGFR2) and Focal Adhesion Kinase (FAK). This compound demonstrates potent inhibitory activity that can suppress angiogenesis and cancer cell proliferation. Research applications include studying tumor growth and metastasis in various cancer models. -
FAK Inhibitor
FAK Inhibitor 5 is a novel allosteric inhibitor of focal adhesion kinase (FAK) that exhibits efficient modulation of FAK activity with IC50 values in the low micromolar range. This compound is utilized in research focusing on cancer biology, cell adhesion, and migration, making it a valuable tool for studying pathways involving FAK signaling. Its specificity allows for detailed investigations into the role of FAK in various cellular processes and disease states. -
PTK2/FAK PROTAC Degrader
BI-0319 is a selective PROTAC degrader targeting PTK2/FAK, effectively promoting the degradation of these proteins. This compound has demonstrated the ability to reduce cancer cell viability, inhibit cellular proliferation, and curtail invasion, making it a valuable tool for cancer research, particularly in studies related to liver cancer. BI-0319 provides insights into therapeutic strategies focused on protein degradation in oncology. -
FAK Inhibitor
FAK-IN-16 is a selective inhibitor of focal adhesion kinase (FAK) that exhibits an exceptionally low IC50 of 1.2 pM. This compound effectively inhibits FAK phosphorylation at both pFAK[Y397] and pFAK[Y861], resulting in decreased tumor growth and reduced vascularity and invasiveness. Additionally, FAK-IN-16 enhances the effects of Cisplatin on tumor cell proliferation and apoptosis in vitro, as well as its anti-tumor properties in murine models. This reagent is valuable for researchers focusing on cancer therapy and tumor biology. -
FAK Inhibitor
FAK-IN-8 is a potent inhibitor of Focal Adhesion Kinase (FAK) with an IC50 value of 5.32 µM. It exhibits significant anti-proliferative activity, making it a valuable tool for cancer research. This compound can be utilized to explore the role of FAK in tumor progression and metastasis, as well as in the development of targeted therapies.
