Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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 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
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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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
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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multi-kinase inhibitor
Conteltinib (CT-707) is a multi-kinase inhibitor targeting FAK, ALK, and Pyk2. Conteltinib (CT-707) exerts significant inhibitory effect on FAK with an IC50 of 1.6 nM. -
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
Defactinib (VS-6063; PF-04554878) is a novel FAK inhibitor with potential antiangiogenic and antineoplastic activities. -
FAK inhibitor
Defactinib hydrochloride (VS-6063 hydrochloride; PF 04554878 hydrochloride) is a novel FAK inhibitor, which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner. -
FAK and Pyk2 kinase inhibitor
PF-562271 hydrochloride is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC50s of 1.5 nM and 13 nM, respectively. -
FAK inhibitor
Ifebemtinib (BI-853520, IN-10018) is an orally active and potent inhibitor of focal adhesion kinase (FAK), with an IC50 of 1 nM against recombinant FAK. It exhibits antiproliferative activity in cancer cells and also inhibits FER and FES kinases, with IC50 values of 900 nM and 1040 nM, respectively. -
Hsp90/HSV inhibitor
AT-533 is a potent inhibitor of heat shock protein 90 (Hsp90) and herpes simplex virus (HSV), exhibiting strong antitumor and antiviral activities. It suppresses tumor growth and angiogenesis by disrupting the HIF-1α/VEGF/VEGFR-2 signaling axis, a critical pathway in tumor vascularization and progression. Additionally, AT-533 inhibits key downstream signaling cascades, including Akt/mTOR/p70S6K, ERK1/2, and FAK pathways. In endothelial cells, specifically human umbilical vein endothelial cells (HUVECs), AT-533 effectively inhibits tube formation, cell migration, and invasion, highlighting its anti-angiogenic properties. These combined effects position AT-533 as a promising candidate for cancer therapy and angiogenesis-related disease research. -
NF-κB/FAK/MAPK inhibitor
Keracyanin chloride is an orally active anthocyanin compound with potent antioxidant, anti-inflammatory, and hypoglycemic properties. It exerts its biological effects by inhibiting the NF-κB/FAK/MAPK signaling pathways, which are central to inflammation, cell adhesion, and metabolic regulation. -
PROTAC FAK Degrader
GSK215 is a potent and selective PROTAC degrader targeting focal adhesion kinase (FAK) via the VHL E3 ligase. With a pDC50 of 8.4, it induces rapid and sustained degradation of FAK, leading to significant modulation of FAK levels over time. This compound demonstrates an extended pharmacokinetic/pharmacodynamic disconnect, making it a valuable tool for research applications in cancer biology and signaling pathways associated with cell adhesion and migration. -
FAK Inhibitor
FAK Inhibitor 7 is a potent focal adhesion kinase (FAK) inhibitor with an IC50 of 3.58 nM. This compound disrupts downstream signaling pathways associated with FAK, including Src and AKT, leading to cell cycle arrest in the G0/G1 phase and promoting cytotoxic autophagy in ovarian cancer cells. Additionally, FAK Inhibitor 7 has demonstrated efficacy in inhibiting tumor metastasis and growth in preclinical ovarian cancer mouse models, making it a valuable tool for studying cancer biology and therapeutic interventions. -
FAK Inhibitor
FAK-IN-22 is a selective inhibitor of focal adhesion kinase (FAK) with additional activity against JAK3 and Aurora B, exhibiting IC50 values of 50.94 nM, 9.99 nM, and 0.49 nM, respectively. This compound demonstrates significant anti-tumor effects in pancreatic ductal adenocarcinoma (PDAC) by inhibiting cell proliferation, inducing apoptosis, and causing G2/M phase arrest in PANC-1 cells, with an IC50 of 0.15 μM. FAK-IN-22’s action is primarily mediated through the inhibition of the FAK/PI3K/Akt signaling pathway, making it a valuable tool for studying cancer cell dynamics and signaling mechanisms. -
FAK Inhibitor
FAK-IN-20 is a potent Focal Adhesion Kinase (FAK) inhibitor with an IC50 value of 0.27 nM. This compound demonstrates significant anticancer activity by inducing apoptosis and generating reactive oxygen species (ROS). Additionally, FAK-IN-20 is effective in arresting the cell cycle in the G2/M phase, making it a valuable tool for research in cancer biology and therapeutic strategies targeting FAK signaling pathways. -
FAK/FGFR2 Inhibitor
PHM16 is an ATP-competitive inhibitor targeting Focal Adhesion Kinase (FAK) and Fibroblast Growth Factor Receptor 2 (FGFR2), with IC50 values of 0.4 μM and 0.37 μM, respectively. This compound exhibits strong anti-angiogenic properties, making it a valuable tool for studies focused on inhibiting tumor angiogenesis and understanding related signaling pathways. Its dual inhibition profile positions PHM16 as an important reagent for cancer research and therapeutic development targeting angiogenesis-related mechanisms. -
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.
