FAK

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 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-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.

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.

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-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-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-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-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.

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-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-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-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 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.

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 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.

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-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-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.

FAK/Aurora kinase-IN-1 is a dual inhibitor targeting focal adhesion kinase (FAK) and Aurora kinase, exhibiting IC50 values of 6.61 nM and 0.91 nM, respectively. This compound demonstrates significant anticancer activity, making it a valuable tool for research applications focused on cancer biology and therapeutic development. Its efficacy in inhibiting both kinases positions it as a promising candidate for further studies in tumor proliferation and treatment strategies.

FAK-IN-10 is a potent inhibitor of focal adhesion kinase (FAK) with an IC50 of 76.3 µM. This compound demonstrates significant antitumor activity, particularly against the MCF-7 and A431 cell lines, exhibiting IC50 values of 4.23 µM and 0.78 µM, respectively. FAK-IN-10 is valuable for research focused on cancer therapeutics and the modulation of signaling pathways associated with tumor growth and metastasis.