2. Signaling Pathways
  3. Protein Tyrosine Kinase/RTK
  4. FAK

FAK

PTK2 protein tyrosine kinase 2; PTK2; Focal adhesion kinase

FAK

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FAK (Focal Adhesion Kinase or PTK2) is a non-receptor and non-membrane associated protein tyrosine kinase that is activated at the sites of cell-matrix adhesions and integrin clustering by auto-phosphorylation (at Tyr397), Src, and other tyrosine kinases. FAK mediates integrin-based cell signaling by transferring signals regulating cell migration, adhesion, and survival from the extracellular matrix to the cytoplasm.

FAK is overexpressed in many tumors, including those derived from the head and neck, colon, breast, prostate, liver, and thyroid. Furthermore, FAK overexpression is highly correlated with an invasive phenotype in these tumors. Inhibition of FAK signaling by overexpression of dominant-negative fragments of FAK reduces invasion of glioblastomas and ovarian cancer cells. FAK therefore represents an important target for the development of anti-neoplastic and anti-metastatic drugs.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-163121
    PST3.1a
    		Inhibitor
    PST3.1a is an orally active and brain-penetrant N-acetylglucosamine glycosyltransferase (MGAT5) inhibitor with a human IC50 of 2 µM. PST3.1a inhibits TGFβR and FAK signaling pathway activity. PST3.1a alters β1,6-GlcNAc N-glycans and microtubule/microfilament integrity, increases OLIG2 expression, and inhibits proliferation, migration, invasiveness, and clonogenic capacities of glioblastoma initiating cells. PST3.1a reduces invasive and proliferative capacity of glioblastoma initiating cells in orthotopic graft models, increases overall survival of orthotopic graft model mice. PST3.1a blunts MGAT5 overexpression, decreases renal fibrosis via collagen 1, collagen 4, and galectin 3 downregulation in a rat chronic kidney disease model. PST3.1a can be used for the research of glioblastoma multiforme and chronic kidney disease.
    PST3.1a
  • HY-170936
    MY-1576
    		Inhibitor
    MY-1576 is a FAK inhibitor with an IC50 of 8 nM. MY-1576 can activate the Hippo pathway, thereby blocking the regulation of YAP/TAZ. MY-1576 also effectively inhibits tumor growth in the KYSE30 xenograft mouse model, demonstrating good safety, and effectively downregulates the autophosphorylation of FAK and the levels of YAP/TAZ in vivo.
    MY-1576
  • HY-145108
    FAK-IN-1
    		Inhibitor
    FAK-IN-1 is a FAK inhibitor with anticancer activities (WO2020231726 (Example 27)).
    FAK-IN-1
  • HY-N1983R
    Caudatin (Standard)
    Caudatin (Standard) is the analytical standard of Caudatin (HY-N1983). This product is intended for research and analytical applications. Caudatin is an orally active and brain-penetrant C-21 steroidal found in Cynanchum bungei decne with a variety of biological activities. Caudatin can inhibit cell proliferation, migration, invasion, cause cell phase arrest, induce apoptosis, autophagy, ROS prodution and loss of mitochondrial membrane potential. Caudatin activates PARP, caspase-3, -7, -9, upregulates pro-apoptotic Bad and Bax and downregulates anti-apoptotic Bcl-2 and Bcl-XL. Caudatin suppresses VEGF, FAK phosphorylation, upregulates p21, p27, DR5 protein expression, activates the p38 MAPK, JNK and PPARα/TFEB-mediated autophagy-lysosomal signaling pathways. Caudatin can be used for the research of cancer, inflammation and neurological disease, such as glioma and Alzheimer's disease.
    Caudatin (Standard)
  • HY-15357
    ALK inhibitor 1
    		Inhibitor 99.16%
    ALK inhibitor 1 (compound 17) is a potent pyrimidin ALK inhibitor. ALK inhibitor 1 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC50=31 nM) and focal adhesion kinase (FAK; IC50=2 nM).
    ALK inhibitor 1
  • HY-44146
    Defactinib analogue-1
    Defactinib analogue-1 (Compound 7) is a ligand for target protein Fak, that can be used for synthesis of PROTAC FAK degrader 1 (HY-119932).
    Defactinib analogue-1
  • HY-A0280
    Roslin 2 bromide
    		99.0%
    Roslin 2 bromide (Benzylhexamethylenetetramine bromide) is a p53 reactivator with anticancer effects. Roslin 2 bromide binds FAK, disrupts the binding of FAK and p53.
    Roslin 2 bromide
  • HY-122672
    Adhesamine
    		Activator 99.46%
    Adhesamine, dumbbell-shaped molecule, activates MAPK/FAK pathway. Adhesamine promotes adhesion and growth of mammalian cells. Adhesamine accelerates the differentiation and improves the survival of mice hippocampal neurons in primary culture.
    Adhesamine
  • HY-161358
    FAK-IN-20
    		Inhibitor
    FAK-IN-20 (Compound 7b) is an inhibitor of FAK with an IC50 value of 0.27 nM. FAK-IN-20 exhibits anticancer activity. FAK-IN-20 can arrest the cell cycle in the G2/M phase and induce cell apoptosis by generating ROS.
    FAK-IN-20
  • HY-143458
    FAK PROTAC B5
    		Inhibitor
    FAK PROTAC B5 (Compound B5) is a FAK PROTAC degrader with an IC50 value of 14.9 nM. FAK PROTAC B5 presents strong FAK degradation activity, antiproliferative activity, outstanding plasma stability and moderate membrane permeability. FAK PROTAC B5 inhibits cell migration and invasion.
    FAK PROTAC B5
  • HY-171009
    FAK-IN-23
    		Inhibitor
    FAK-IN-23 (Compound II) is the inhibitor for focal adhesion kinase (FAK).
    FAK-IN-23
  • HY-117595
    PHM16
    		Inhibitor
    PHM16 is an ATP competitive inhibitor of FAK and FGFR2 (IC50: 0.4 μM and 0.37 μM, respectively), with direct potent anti-angiogenic activity.
    PHM16
  • HY-P5929
    VnP-16
    		Inducer
    VnP-16 can promote bone formation by accelerating osteoblast differentiation and activity through direct interaction with β1 integrin followed by FAK activation.
    VnP-16
  • HY-183123
    EGFR T790M/FAK-IN-1
    		Inhibitor
    EGFR T790M/FAK-IN-1 is a dual inhibitor of EGFRT790M and FAK, with an IC50 of 99.1 nM against EGFRT790M and an IC50 of 117.7 nM against FAK. EGFR T790M/FAK-IN-1 can be used for research on pancreatic cancer, drug-resistant breast cancer, and drug-resistant lung cancer.
    EGFR T790M/FAK-IN-1
  • HY-155440
    FAK-IN-15
    		Inhibitor
    FAK-IN-15 (Compound 9b) is a focal adhesion kinase (FAK) inhibitor with an IC50 value of 0.2691 nM. FAK-IN-15 has anti-tumor activity with an IC50 value of 1.033 μM against U87-MG cells.
    FAK-IN-15
  • HY-116497
    PH11
    		Inhibitor
    PH11 is a novel focal adhesion kinase (FAK) inhibitor that rapidly induces apoptosis in TRAIL-resistant PANC-1 cells when combined with TRAIL, but has no effect on normal human fibroblasts. The study found that PH11 downregulates c-FLIP through inhibition of FAK and phosphatidylinositol-3-kinase (PI3K)/AKT pathways, thereby restoring the TRAIL apoptotic pathway, suggesting that this combination therapy may provide an attractive therapeutic strategy for the safe and effective treatment of pancreatic cancer. PH11 selectively inhibits c-FLIP expression by modulating upstream signaling pathways and may represent an innovative therapeutic strategy. Although further work is needed to fully elucidate the mechanism of PH11-induced TRAIL sensitization, we believe that our results will provide a new approach to target c-FLIP without the risk of interfering with caspase-8 processing, which could potentially lead to TRAIL resistance. This study also suggests a role for the FAK/AKT signaling pathway in regulating c-FLIP expression in TRAIL-induced apoptosis, and this understanding will provide important clues to control the resistance mechanism to optimize the potential of TRAIL-based pancreatic cancer treatment.
    PH11
  • HY-173495
    FAK-IN-25
    		Inhibitor
    FAK-IN-25 (4c) is a FAK inhibitor with an IC50 of 50.98 nM. FAK-IN-25 (4c) induces apoptosis and causes cell cycle arrest at G1 phase. FAK-IN-25 (4c) can be used in cancer research.
    FAK-IN-25
  • HY-109582S
    ADT-OH-d4
    ADT-OH-d4 (ACS 1-d4) is the deuterium labeled ADT-OH (HY-109582). ADT-OH is a hydrogen sulfide-releasing donor. ADT-OH induces apoptosis and upregulates FADD. ADT-OH inhibits FAK/Paxillin. ADT-OH has the potential for the research of cancer diseases.
    ADT-OH-d<sub>4</sub>
  • HY-175459
    PROTAC FAK degrader 3
    		Degrader
    PROTAC FAK degrader 3 is a selective FAK PROTAC degrader (DC50 = 1.08 nM). PROTAC FAK degrader 3 induces FAK degradation dependent on the ubiquitin-proteasome system and its binding to FAK and CRBN. PROTAC FAK degrader 3 upregulates MHC-I gene transcription and tumor cell surface expression by inhibiting the non-catalytic activity of FAK, leading to increased antigen presentation and activation of cytotoxic CD8 T cells. PROTAC FAK degrader 3 enhances in vivo anti-tumor activity by promoting MHC-I expression and enhancing T cell activation. PROTAC FAK degrader 3 can be used in cancer research targeting FAK degradation in ovarian cancer, hepatocellular carcinoma, and other cancers. (Pink: FAK-IN-3:HY-143407, Blue: Thalidomide-4-OH:HY-103596, Blue + Black: FAK ligand-3: HY-W939883, Black: Linker).
    PROTAC FAK degrader 3
  • HY-183697
    FAK-IN-30
    		Inhibitor
    FAK-IN-30 is a focal adhesion kinase (FAK) inhibitor with moderate cytotoxicity against breast cancer cells. FAK-IN-30 can be used for the research of triple-negative breast cancer.
    FAK-IN-30
Cat. No. Product Name / Synonyms Application Reactivity