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-172888
    SPP-037
    		Inhibitor
    SPP-037 is an orally active and selective inhibitor of ST6GAL1 (IC50 = 3.59 μM). SPP-037 inhibits integrin α2,6-sialylation and integrin-FAK-paxillin pathway. SPP-037 inhibits cancer cell proliferation, migration and exhibits antiangiogenic activity. SPP-037 has anti-tumor activity in MDA-MB-231 xenograft mouse model. SPP-037 can be used for the research of triple-negative breast cancer.
    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-179512
    BSJ-04-146
    		Degrader
    BSJ-04-146 is a highly efficient and selective PROTAC targeting focal adhesion kinase (FAK) inhibitor(IC50 = 26 nM). BSJ-04-146 achieves rapid and potent FAK degradation with high proteome-wide specificity in cancer cells and induces durable degradation in mice. BSJ-04-146 binds FAK and requires the ubiquitin-proteasome machinery to achieve FAK degradation. BSJ-04-146 can be used for the study of pancreatic cancer and triple-negative breast cancer.
    BSJ-04-146
  • 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-183284
    GZD-552
    		Inhibitor
    GZD-552 is a potent orally active FAK inhibitor with a human FAK IC50 of 5.8 nM. GZD-552 suppresses FAK phosphorylation activation and downstream ERK signaling. GZD-552 induces apoptosis and G2/M cell cycle arrest, and exhibits antiproliferative activities in glioblastoma multiforme cells. GZD-552 exhibits antitumor efficacy in mice xenograft model. GZD-552 can be used for the research of glioblastoma multiforme.
    GZD-552
  • HY-E70716
    FAK aa411-686 Recombinant Human Active Protein Kinase
    Focal adhesion kinase (FAK), a non-receptor tyrosine kinase in the cytoplasm, couples with integrins and growth factor receptors to regulate cell adhesion, proliferation, migration, invasion, and metastasis. FAK is overexpressed and aberrantly activated in many cancer types, including triple negative breast cancer (TNBC). FAK aa411-686 Recombinant Human Active Protein Kinase is a recombinant FAK aa411-686 protein that can be used to study FAK aa411-686-related functions.
    FAK aa411-686 Recombinant Human Active Protein Kinase
  • 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-178467
    PROTAC FAK degrader 4
    		Degrader
    PROTAC FAK degrader 4 (Compound 9C) is an efficient and selective FAK PROTAC degrader. PROTAC FAK degrader 4 has a DC50 of 3.6 nM in MDA-MB-231 cells. PROTAC FAK degrader 4 significantly inhibits tumor cell proliferation, migration, and invasion, and enhances chemotherapy sensitivity to cisplatin (HY-17394). PROTAC FAK degrader 4 can be used for research on cancer. (Pink: FAK Ligand (HY-43760); Blue: VHL Ligand (HY-125845); Black: Linker (HY-W208616))
    PROTAC FAK degrader 4
  • 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-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-E71029
    Active focal adhesion kinase, Human
    Active focal adhesion kinase, Human (EC 2.7.10.2) is a cytoplasmic protein tyrosine kinase which is found concentrated in the focal adhesions that form between cells growing in the presence of extracellular matrix constituents.
    Active focal adhesion kinase, Human
  • HY-N17888
    Ephemeranthol A
    		Inhibitor
    Ephemeranthol A is a phenanthrene compound with anticancer and anti-inflammatory activities. Ephemeranthol A exerts significant anti-inflammatory effects in macrophages by inhibiting the NF-κB and MAPK signaling pathways. Ephemeranthol A induces apoptosis and inhibits metastasis of lung cancer cells by suppressing the FAK/Akt signaling and EMT processes. Ephemeranthol A can be used for the research of acute and chronic inflammatory diseases and non-small cell lung cancer.
    Ephemeranthol A
  • 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-160411
    FAK-IN-18
    		Inhibitor
    FAK-IN-18 is a focal adhesion kinase (FAK) inhibitor with an IC50 of .84 nM. FAK-IN-18 can be used for the research of gastric cancer.
    FAK-IN-18
  • HY-183784
    P2X7R antagonist-1
    		Inhibitor
    P2X7R antagonist-1 is an orally active P2X7 receptor antagonist with an IC50 of 3.57 μM. P2X7R antagonist-1 inhibits the proliferation, invasion and metastasis abilities of cancer cells. P2X7R antagonist-1 downregulates the expression of FAK and MMP-9. P2X7R antagonist-1 suppresses tumor growth and metastasis in a mouse breast cancer model. P2X7R antagonist-1 promotes the activation of CD4 and CD8 T cells. P2X7R antagonist-1 can be used in breast cancer-related research.
    P2X7R antagonist-1
Cat. No. Product Name / Synonyms Application Reactivity