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-P10323
    T7 Peptide
    		Inhibitor
    T7 Peptide is a protein synthesis inhibitor and anti-angiogenic agent, with a Kd of 10 nM for human transferrin receptor. T7 Peptide inhibits the phosphorylation of focal adhesion kinase, the activation of phosphatidylinositol 3-kinase and Akt, the kinase activity of mTOR, as well as the phosphorylation of 4E-BP1 in endothelial cells. T7 Peptide induces G0/G1 cell cycle arrest, apoptosis and protective autophagy in hepatocellular carcinoma cells, and suppresses tumor growth in mouse models. T7 Peptide is applicable to research related to cancer, glioblastoma, hepatocellular carcinoma and glioma.
    T7 Peptide
  • HY-148110
    FAK-IN-8
    		Inhibitor
    FAK-IN-8 (compound 5h) is a FAK inhibitor (IC50=5.32 µM). FAK-IN-8 has good anti-proliferative activity and can be used in cancer research.
    FAK-IN-8
  • HY-10458R
    PF-562271 besylate (Standard)
    		Inhibitor
    PF-562271 besylate (Standard) is the analytical standard of PF-562271 besylate (HY-10458). This product is intended for research and analytical applications. PF-562271 (VS-6062) besylate is a potent ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase, with an IC50 of 1.5 nM and 13 nM, respectively.
    PF-562271 besylate (Standard)
  • HY-109582R
    ADT-OH (Standard)
    ADT-OH (Standard) is the analytical standard of ADT-OH. This product is intended for research and analytical applications. 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 (Standard)
  • HY-N15267
    Ovalitenone
    		Inhibitor
    Ovalitenone is a flavonoid compound that can be isolated from the plant Millettia peguensis. It shows no cytotoxic effects on lung cancer H460 and A549 cells, but it significantly inhibits anchorage-independent growth, CSC-like phenotypes, colony formation, and the migration and invasion capabilities of cancer cells. Ovalitenone can significantly reduce the levels of N-cadherin, snail, and slug, while increasing E-cadherin, thus inhibiting the EMT pathway. Additionally, Ovalitenone suppresses the signaling pathways regulated by focal adhesion kinase (FAK), ATP-dependent tyrosine kinase (AKT), mammalian target of rapamycin (mTOR), and cell division cycle 42 (Cdc42).
    Ovalitenone
  • HY-13203R
    NVP-TAE 226 (Standard)
    		Inhibitor
    NVP-TAE 226 (Standard) is the analytical standard of NVP-TAE 226. This product is intended for research and analytical applications. NVP-TAE 226 (TAE226) is a potent and ATP-competitive dual FAK and IGF-1R inhibitor with IC50s of 5.5 nM and 140 nM, respectively. NVP-TAE 226 (TAE226) also effectively inhibits Pyk2 and insulin receptor (InsR) with IC50s of 3.5 nM and 44 nM, respectively.
    NVP-TAE 226 (Standard)
  • HY-100498R
    GSK2256098 (Standard)
    		Inhibitor
    GSK2256098 (Standard) is the analytical standard of GSK2256098 (HY-100498). This product is intended for research and analytical applications. GSK2256098 is a selective FAK kinase inhibitor, which inhibits growth and survival of pancreatic ductal adenocarcinoma cells.
    GSK2256098 (Standard)
  • HY-10460R
    PF-431396 (Standard)
    		Inhibitor
    PF-431396 (Standard) is the analytical standard of PF-431396 (HY-10460). This product is intended for research and analytical applications. PF-431396 is an orally active dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor, with IC50 values of 2 nM and 11 nM, respectively.
    PF-431396 (Standard)
  • HY-160447
    FAK/Aurora kinase-IN-1
    		Inhibitor
    FAK/Aurora kinase-IN-1 is a FAK and aurora kinase inhibitor with IC50 values of 6.61 nM and 0.91 nM, respectively. FAK/Aurora kinase-IN-1 shows anticancer effects (WO2018019252A1; compound 11).
    FAK/Aurora kinase-IN-1
  • HY-169517
    Protein kinase inhibitor 10
    		Inhibitor
    Protein kinase inhibitor 10 is a protein kinase inhibitor with IC50 values of 28.9, 13.6, and 2.41 μM for TAM receptor, FAK, and KIT, respectively. Protein kinase inhibitor 10 can inhibit abnormal and excessive cell proliferation, showing promise for research in cancer therapy.
    Protein kinase inhibitor 10
  • HY-10459R
    PF-562271 (Standard)
    		Inhibitor
    PF-562271 (Standard) is the analytical standard of PF-562271 (HY-10459). This product is intended for research and analytical applications. PF-562271 (VS-6062) is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC50s of 1.5 nM and 13 nM, respectively.
    PF-562271 (Standard)
  • HY-160187A
    (Rac)-AAA
    		Inhibitor 99.02%
    (Rac)-AAA is a regulator and inhibitor targeting GPR75. By blocking the 20-HETE-induced downregulation of GPR75 expression, (Rac)-AAA effectively inhibits the activation of key downstream signaling pathways including EGFR, AKT, NF-κB and FAK. (Rac)-AAA reverses 20-HETE-mediated epithelial-mesenchymal transition, which is specifically characterized by downregulating vimentin (vimentin), upregulating E-Cadherin, as well as reducing MMP-2 activity and cancer cell migration ability. (Rac)-AAA also abolishes the 20-HETE-induced upregulation of HIC-5 expression and anchorage-independent growth, and modulates the subcellular localization of PKC-α and phosphorylated AKT. (Rac)-AAA is investigated in androgen-independent prostate cancer (castration-resistant prostate cancer).
    (Rac)-AAA
  • HY-164527
    Si306
    		Inhibitor
    Si306 is a Src inhibitor with antitumor activity. Si306 reduces the phosphorylation of focal adhesion kinase (FAK) and the expression of epidermal growth factor receptor (EGFR), and inhibits the invasion of human glioblastoma (GBM).
    Si306
  • HY-105174AR
    BPC 157 acetate (Standard)
    		Activator
    BPC 157 acetate (Standard) is the analytical standard of BPC 157 acetate (HY-105174A). This product is intended for research and analytical applications. BPC 157 acetate is the acetate salt form of BPC 157 (HY-105174). BPC 157 acetate is the 15-amino acide fragment of gastric peptide BPC. BPC 157 acetate exhibits wound healing promoting and neuroprotective activity. BPC 157 acetate maintains the integrity of the gastrointestinal mucosa without significant toxicity. BPC 157 acetate counteracts NSAIDs/insulin overdose/copper-induced toxicity. BPC 157 acetate ameliorates specific (over)stimulated/damaged neurotransmitter systems-induced behavioral disorders through serotonergic and dopaminergic systems.
    BPC 157 acetate (Standard)
  • HY-153697
    FAK-IN-10
    		Inhibitor 98.04%
    FAK-IN-10 is an inhibitor of FAK with an IC50 of 76.3 μM. FAK-IN-10 exhibits antitumor activity against MCF-7 and A431 cell lines with IC50s of 4.23 and 0.78 μM,respectively.
    FAK-IN-10
  • HY-12289R
    Defactinib (Standard)
    		Inhibitor
    Defactinib (Standard) is the analytical standard of Defactinib. This product is intended for research and analytical applications. Defactinib (VS-6063; PF-04554878) is a novel FAK inhibitor with potential antiangiogenic and antineoplastic activities.
    Defactinib (Standard)
  • HY-105935R
    Keracyanin chloride (Standard)
    		Inhibitor
    Keracyanin (chloride) (Standard) is the analytical standard of Keracyanin (chloride). This product is intended for research and analytical applications. Keracyanin chloride inhibits NF-κB/FAK/MAPK signaling pathway. Keracyanin chloride exhibits antioxidant, anti-inflammatory and hypoglycemic effects, and is orally active.
    Keracyanin chloride (Standard)
  • HY-122585
    proMMP-9 inhibitor-3c
    		Inhibitor
    proMMP-9 inhibitor-3c (compound 3c) is a potent proMMP-9 inhibitor. proMMP-9 inhibitor-3c is specific for binding to the proMMP-9 hemopexin-like domain (Kd=320 nM). proMMP-9 inhibitor-3c disruption of MMP-9 homodimerization prevents association of proMMP-9 with both α4β1 integrin and CD44 and results in the dissociation of EGFR. This disruption results in decreased phosphorylation of Src and its downstream target proteins focal adhesion kinase (FAK) and paxillin (PAX).
    proMMP-9 inhibitor-3c
  • HY-183946
    NVP-TAC544
    		Inhibitor
    NVP-TAC544 is a focal adhesion kinase (FAK) inhibitor. NVP-TAC544 inhibits angiogenesis. NVP-TAC544 can be used for the research of melanoma (primary or metastatic).
    NVP-TAC544
  • HY-10209R
    Masitinib (Standard)
    		Inhibitor
    Masitinib (Standard) is the analytical standard of Masitinib. This product is intended for research and analytical applications. Masitinib (AB1010) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib (AB1010) has anti-proliferative, pro-apoptotic activity and low toxicity.
    Masitinib (Standard)
Cat. No. Product Name / Synonyms Application Reactivity