Catalog No.
Product Name
Application
Product Information
Citations
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FAK Inhibitor
PF 573228 is a potent and selective inhibitor of focal adhesion kinase (FAK) (IC50 = 4 nM).- Dagyeong Lee, .et al. , J Transl Med, 2024, Feb 14;22(1):154 PMID: 38355577
- Izumi D, .et al. , Int J Cancer, 2016, Mar 1;138(5):1207-19 PMID: 26414794
- Aya Yokota-Nakatsuma, .et al. , Sci Rep, 2016, 6: 37914 PMID: 27897208
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FAK inhibitor
PF-00562271 is the benzenesulfonate salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK and Pyk2 with IC50 of 1.5 nM and 14 nM, respectively.- Dai Sonoda, .et al. , Oncol Rep, 2022, Jan;47(1):19 PMID: 34796907
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FAK inhibitor
PF-562271 is an orally bioavailable small molecule and ATP-competitive focal adhesion kinase (FAK) inhibitor with potential antineoplastic and antiangiogenic activities.- Jiping Yue, .et al. , Nat Commun, 2016, 7: 11692 PMID: 27216888
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FAK inhibitor
PF-04554878 is a novel FAK kinase inhibitor that decreases growth and induces apoptosis in pancreatic neuroendocrine tumor cells- Shalana O'Brien, .et al. , Oncotarget., 2014, Sep; 5(17): 7945-7959 PMID: 25277206
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FAK inhibitor
NVP-TAE226 is a potent FAK inhibitor with IC50 of 5.5 nM and modestly potent to Pyk2(IC50=3.5 nM); 10- to 100-fold less potent against InsR, IGF-1R, ALK, and c-Met.- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
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Aurora A/B Kinase inhibitor
PF-03814735 is a novel, potent and reversible inhibitor of Aurora A/B with IC50of 0.8 nM/5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1. Phase 1. -
PYK2/FAK inhibitor
PF-4618433 shows improved PYK2 potency, reduced p38 activity, and superior overall selectivity relative to the prototype BIRB796. -
FAK inhibitor
GSK2256098 is a focal adhesion kinase-1 (FAK) inhibitor with potential antiangiogenic and antineoplastic activities. -
FAK degrader
PROTAC FAK degrader 1 is a selective and potent focal adhesion kinase (Fak) degrader with an IC50 of 6.5 nM, DC50 of 3 nM. -
FAK Inhibitor
PND-1186 hydrochloride is a potent and selective inhibitor of Focal Adhesion Kinase (FAK) with an IC50 value of 1.5 nM. This reversible inhibitor has been shown to promote apoptosis in tumor cells, making it a valuable tool in cancer research. PND-1186 hydrochloride is applicable in investigations aimed at understanding FAK's role in tumor progression and therapeutic resistance. -
ALK/FAK/ROS1 Multikinase Inhibitor
APG-2449 is an orally active inhibitor targeting BCL-2 and multikinase pathways, specifically ALK, FAK, and ROS1. It demonstrates potent antitumor activity by reducing cell viability and enhancing apoptosis in acute myeloid leukemia cells in vitro. APG-2449 effectively decreases the activation of FAK and its downstream signaling effectors. This compound is suitable for research applications in various malignancies, including mesothelioma, non-small cell lung cancer, ovarian cancer, and other hematologic and solid tumors. -
FAK Inhibitor
YH-306 is a selective FAK (Focal Adhesion Kinase) inhibitor that exhibits potent antitumor activity. It effectively suppresses colorectal tumor growth and metastasis by inhibiting key signaling pathways, leading to significant reductions in the migration and invasion of colorectal cancer cells. YH-306 also induces apoptosis and inhibits the proliferation of cancer cells by disrupting the activation of FAK, c-Src, paxillin, and downstream effectors such as PI3K and Rac1, while downregulating MMP2 and MMP9 expression. Additionally, this compound impedes actin polymerization mediated by the Arp2/3 complex, contributing to its antitumor effects. -
FAK Inhibitor
GSK-2256098 hydrochloride is a selective inhibitor of focal adhesion kinase (FAK), known for its antiangiogenic and antineoplastic properties. By targeting FAK, it effectively disrupts tumor cell growth through the modulation of key cellular processes, including adhesion, migration, proliferation, and survival. This compound is valuable for researchers investigating the mechanisms of cancer progression and the development of potential therapeutic strategies. -
FAK Inhibitor
FAK-IN-2 is a potent inhibitor of focal adhesion kinase (FAK), exhibiting a reported IC50 of 35 nM. This compound effectively covalently modifies and inhibits the autophosphorylation of FAK, leading to significant inhibition of tumor cell migration and clonal formation. Additionally, FAK-IN-2 induces apoptosis in cancer cells, highlighting its potential utility in oncological research and therapeutic applications targeting FAK signaling pathways. -
FAK Signaling Inhibitor
FAK-IN-5 is a potent inhibitor of focal adhesion kinase (FAK) signaling. It effectively induces apoptosis and autophagy in various cell types, making it a valuable tool for studying cellular responses to FAK modulation. This compound is utilized in cancer research and investigations related to cell migration and survival pathways. -
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. -
FAK Inhibitor
FAK-IN-4 is a potent inhibitor of focal adhesion kinase (FAK), a key regulator of cellular adhesion and signaling pathways in cancer. This compound exhibits significant anti-cancer properties, including the induction of apoptosis in various cancer cell lines. FAK-IN-4 is valuable for research applications focused on cancer biology, particularly in studying the modulation of FAK-related signaling pathways and their role in tumor progression. -
NF-κB/MAPK/FAK/Akt Inhibitor
Ephemeranthol A is an inhibitor of NF-κB, MAPK, FAK, and Akt signaling pathways. This phenanthrene compound demonstrates notable anti-inflammatory effects through the inhibition of NF-κB and MAPK pathways in macrophages. Additionally, Ephemeranthol A induces apoptosis and inhibits metastasis in non-small cell lung cancer by suppressing FAK/Akt signaling and epithelial-mesenchymal transition (EMT) processes. It is applicable for research into acute and chronic inflammatory diseases as well as non-small cell lung cancer. -
FAK Inhibitor
FAK-IN-24 is a potent inhibitor of focal adhesion kinase (FAK) with an IC50 of 0.815 nM. This compound induces DNA damage and apoptosis, demonstrating significant anti-glioblastoma activity. FAK-IN-24 effectively inhibits the proliferation of glioblastoma cell lines U87-MG and U251, with IC50 values of 15 nM and 20 nM, respectively, and has shown the ability to suppress tumor growth in U87-MG xenograft models. -
FAK Inhibitor
FAK-IN-29 is a potent selective inhibitor of focal adhesion kinase (FAK), exhibiting an IC50 of 0.5 nM. This compound demonstrates significant antitumor activity by inhibiting proliferation and colony formation of MDA-MB-231 cells, as well as inducing cell cycle arrest and apoptosis. FAK-IN-29 is a valuable tool for investigating the role of FAK in various tumors, particularly in the research of triple-negative breast cancer. -
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.
