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-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-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-172888
    SPP-037
    		Inhibitor
    SPP-037 is an orally active and selective inhibitor of ST6GAL1 (IC50: 3.59 μM). SPP-037 exhibits anti-MDA-MB-231 cell migration activity by inhibiting integrin α2,6-sialylation and integrin-FAK-paxillin pathway. SPP-037 has anti-tumor activity in MDA-MB-231 xenograft mouse model. SPP-037 can be used in breast cancer research.
    SPP-037
  • HY-147520
    FAK-IN-5
    		Inhibitor
    FAK-IN-5 (Compound 8l) is a FAK signaling inhibitor. FAK-IN-5 induces cell apoptosis and autophagy.
    FAK-IN-5
  • HY-168513
    ALK-IN-29
    		Inhibitor
    ALK-IN-29 (compound 4c) has a certain inhibitory effect on tyrosine protein kinases ALK, CDK2/CyclinE1 and FAK, among which the strongest inhibitory effect on ALK kinase is 40.63% at a concentration of 10 μM. ALK-IN-29 can be used for anti-cancer research.
    ALK-IN-29
  • HY-144794
    EGFR-IN-46
    		Inhibitor
    EGFR-IN-46 is a potent EGFR and FAK dual inhibitor with IC50s of 20.17 nM, 14.25 nM, respectively. EGFR-IN-46 significantly inhibits the growth of cancer cells. EGFR-IN-46 induces cell apoptosis.
    EGFR-IN-46
  • HY-168718
    FAK-IN-22
    		Inhibitor
    FAK-IN-22 (Compound 26) is an inhibitor of FAK, JAK3, and Aurora B, with IC50 values of 50.94 nM, 9.99 nM, and 0.49 nM, respectively, effectively inhibiting tumor occurrence and metastasis in pancreatic ductal adenocarcinoma (PDAC). FAK-IN-22 effectively inhibits the proliferation of PANC-1 cells, with an IC50 value of 0.15 μM. FAK-IN-22 induces apoptosis and G2/M phase arrest in PANC-1 cells by inhibiting the FAK/PI3K/Akt signaling pathway.
    FAK-IN-22
  • HY-W040971R
    Creosol (Standard)
    		Inhibitor
    Creosol (Standard) (2-Methoxy-4-methylphenol (Standard)) is the analytical standard of Creosol (HY-W040971). This product is intended for research and analytical applications. Creosol (2-Methoxy-4-methylphenol) is an endogenous metabolite that acts as an important chemical intermediate and potential biofuel mainly derived from lignocellulosic biomass. Creosol is blood brain barrier penetrable.
    Creosol (Standard)
  • HY-143407
    FAK-IN-3
    		Inhibitor
    FAK-IN-3 (Compound 36) is a potent inhibitor of focal adhesion kinase (FAK). FAK-IN-3 not only decreases migration and invasion of PA-1 cells, but also reduces expression of MMP-2 and MMP-9. FAK-IN-3 inhibits tumor growth and metastasis, and no obvious adverse effects. FAK-IN-3 has the potential for the research of ovarian cancer.
    FAK-IN-3
  • HY-171955
    LXG6403
    		Inhibitor
    LXG6403 is an orally active and irreversible LOX inhibitor (IC50 = 1.3 μM). LXG6403 is ~3.5-fold more specific for LOX than LOXL2 and does not inhibit LOXL1. LXG6403 inhibits FAK signaling and induces ROS generation and DNA damage, leading to G1 arrest and apoptosis in chemoresistant triple-negative breast cancer (TNBC) cell lines. LXG6403 alters the extracellular matrix (ECM) and collagen structure, reducing collagen cross-linking and deposition, thereby increasing drug penetration and reducing tumor stiffness. LXG6403 overcomes Doxorubicin (HY-15142) resistance in chemoresistant TNBC PDX in vivo and can be used to study high-stiffness resistant tumors.
    LXG6403
  • HY-146065
    FAK-IN-4
    		Inhibitor
    FAK-IN-4 (Compound 7d) is potential FAK inhibitor with anticancer activities. FAK-IN-4 induces cell apoptosis.
    FAK-IN-4
  • HY-163715
    Antitumor agent-165
    		Inhibitor
    Antitumor agent-165 (Compound 10l) is a potent focal adhesion kinase (FAK) inhibitor. Antitumor agent-165 exhibits effective antiproliferative activity against CAPAN-1, PANC-1, PATU-T, SUIT-2, BxPC-3, PDAC-3 and PANC-1 GR with IC50s in the range of 1.04-3.44 μM.
    Antitumor agent-165
  • HY-173515
    FAK-IN-26
    		Inhibitor
    FAK-IN-26 is a BBB-penetrable Focal Adhesion Kinase (FAK) inhibitor (IC50: 0.87 nM). FAK-IN-26 significantly suppresses tumor cell viability, cancer stem cell activity, and cell migration in A549 and SKOV-3 cell lines. FAK-IN-26 has potent anti-cancer activity in A549 and SKOV-3 tumor mice models with tumor inhibition rates of 59.15 % and 57.9 %.
    FAK-IN-26
  • HY-170486
    MLK3-IN-1
    		Inhibitor
    MLK3-IN-1 (Compound 37) is a selective inhibitor for mixed-lineage protein kinase 3 (MLK3) with an IC50 <1 nM. MLK3-IN-1 inhibits FAK with an IC50 of 15.5 μM. MLK3-IN-1 exhibits good metabolic stability in mouse and human liver microsomes.
    MLK3-IN-1
  • HY-161632
    PROTAC EGFR degrader 10
    		Degrader
    PROTAC EGFR degrader 10 (Compound B56) is a PROTAC degrader for epidermal growth factor receptor (EGFR), with DC50 <100 nM. PROTAC EGFR degrader 10 binds CRBN-DDB1 with a Ki of 37 nM. PROTAC EGFR degrader 10 degrades EGFR, focal adhesion kinase (FAK), and RSK1, inhibits the proliferation of BaF3 wild type and EGFR mutants, with IC50 <150 nM.
    PROTAC EGFR degrader 10
  • HY-168899
    FAK-IN-24
    		Inhibitor
    FAK-IN-24 (Compound 9f) is a FAK inhibitor (IC50: 0.815 nM). FAK-IN-24 induces DNA damage and apoptosis. FAK-IN-24 has anti-glioblastoma activity. FAK-IN-24 inhibits proliferation of glioblastoma cell lines U87-MG (IC50 = 15 nM) and U251 (IC50 = 20 nM). FAK-IN-24 inhibits tumor growth in U87-MG xenograft model.
    FAK-IN-24
  • HY-N0498R
    Nitidine chloride (Standard)
    		Inhibitor
    Nitidine (chloride) (Standard) is the analytical standard of Nitidine (chloride). This product is intended for research and analytical applications. Nitidine chloride, a potential anti-malarial lead compound derived from Zanthoxylum nitidum (Roxb) DC, exerts potent anticancer activity through diverse pathways, including inducing apoptosis, inhibiting STAT3 signaling cascade, DNA topoisomerase 1 and 2A, ERK and c-Src/FAK associated signaling pathway. Nitidine chloride inhibits LPS-induced inflammatory cytokines production via MAPK and NF-kB pathway.
    Nitidine chloride (Standard)
  • HY-122844B
    Ifebemtinib tosylate
    		Inhibitor
    Ifebemtinib (tosylate) (BI-853520 (tosylate); IN-10018 (tosylate)) is a highly selective PTK2 kinase inhibitor. Ifebemtinib (tosylate) demonstrates anti-tumor activity. Ifebemtinib (tosylate) inhibits FAK autophosphorylation in prostate carcinoma cells. Ifebemtinib (tosylate) can inhibit spheroid formation and orthotopic tumor growth in vivo. Ifebemtinib (tosylate) can be studied in anticancer research such as solid tumors, breast cancer, and malignant pleural mesothelioma.
    Ifebemtinib tosylate
  • HY-162034
    FAK-IN-17
    		Inhibitor
    FAK-IN-17 is a focal adhesion kinase (FAK) inhibitor. FAK-IN-17 possesses anticancer activity against A549 and MDA-MB-231 cell lines with IC50 values of 130 nM and 94 nM.
    FAK-IN-17
  • HY-160187A
    (Rac)-AAA
    (Rac)-AAA is the racemate of AAA. (Rac)-AAA is an antagonist of 20-HETE receptor. (Rac)-AAA can increase the expression of GPR75 receptor in androgen-insensitive prostate cancer cells. (Rac)-AAA dose-dependently increases p38 phosphorylation. (Rac)-AAA induces a significant decrease in the phosphor-AKT signal in nuclei of cells. (Rac)-AAA mitigates the NF-κB signal in unstimulated cell nuclei. (Rac)-AAA can diminish the membrane associated signal intensity. (Rac)-AAA decreases the FAK phosphorylation induced by 20-HETE.
    (Rac)-AAA
Cat. No. Product Name / Synonyms Application Reactivity