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-B1305R
    Chloropyramine hydrochloride (Standard)
    		Inhibitor
    Chloropyramine hydrochloride (Standard) is the analytical standard of Chloropyramine hydrochloride. This product is intended for research and analytical applications. Chloropyramine hydrochloride is a histamine receptor H1 antagonist which can also inhibit the biochemical function of VEGFR-3 and FAK.
    Chloropyramine hydrochloride (Standard)
  • HY-149259
    FAK-IN-9
    		Inhibitor
    FAK-IN-9 (Compound 8f) is a potent and orally active FAK inhibitor with an IC50 of 27.44 nM. FAK-IN-9 induces triple-negative breast cancer (TNBC) cell apoptosis.
    FAK-IN-9
  • HY-173603
    FAK-IN-27
    		Inhibitor
    FAK-IN-27 (compound 8A) is a potent and selective FAK inhibitor with an IC50 of 4.968 nM. FAK-IN-27 suppresses H1299 cells proliferation with an IC50 of 0.28 μM. FAK-IN-27 can be used in the study of NSCLC.
    FAK-IN-27
  • HY-122844A
    Ifebemtinib hydrochloride
    		Inhibitor
    Ifebemtinib (BI-853520) hydrochloride is an orally active and potent focal adhesion kinase (FAK) inhibitor (IC50 = 1 nM for recombinant FAK). Ifebemtinib hydrochloride exhibits antiproliferative activity against cancer cells.
    Ifebemtinib hydrochloride
  • HY-156334
    FAK-IN-12
    		Inhibitor
    FAK-IN-12 (Compound 12S) is a FAK inhibitor (IC50 = 47 nM). FAK-IN-12 inhibits MGC-803, HCT-116 and KYSE30 cell proliferation (IC50: 0.24, 0.45, 0.44 μM). FAK-IN-12 induces apoptosis and cellular senescence.
    FAK-IN-12
  • HY-156026
    FAK-IN-11
    		Inhibitor
    FAK-IN-11 (Compound 4l) is a FAK inhibitor. FAK-IN-11 binds to the ATP binding pocket of FAK, and inhibits phosphorylation of FAK protein. FAK-IN-11 shows cytotoxic activity against the MDA-MB-231 cells with an IC50 of 13.73? μM. FAK-IN-11 induces non-apoptotic cell death in MDA-MB-231 cells.
    FAK-IN-11
  • HY-162879
    FAK inhibitor 7
    		Inhibitor
    FAK inhibitor 7 is a type of FAK inhibitor with an IC50 value of 3.58 nM. FAK inhibitor 7 can inhibit the downstream signaling cascades of FAK (like Src and AKT), causing ovarian cancer cells to stall in the G0/G1 phase and induce cytotoxic autophagy. FAK inhibitor 7 can also suppress tumor metastasis and growth in ovarian cancer mice.
    FAK inhibitor 7
  • HY-150730
    FAK-IN-6
    		Inhibitor
    FAK-IN-6 is a potent FAK inhibitor with an IC50 value of 1.415 nM. FAK-IN-6 has anti-proliferative activity against certain cancer cell lines. FAK-IN-6 can be used for researching pancreatic cancer.
    FAK-IN-6
  • HY-146203
    FAK inhibitor 6
    Compound 26F not only optimized the effective inhibitory enzyme (ic50= 28.2 nm), but also showed relatively less cytotoxicity (ic50= 3.32 μ M) And induced MDA-MB-231 cell apoptosis in a dose-dependent manner, effectively blocking MDA-MB-231 cells in g0/g1 phase.
    FAK inhibitor 6
  • HY-157965
    ZINC09875266
    		Inhibitor
    ZINC09875266 is a dual inhibitor targeting VEGFR2 and FAK that can be used in cancer research.
    ZINC09875266
  • HY-18928
    FAK inhibitor 5
    		Inhibitor
    FAK inhibitor 5 (compound 2) is a novel allosteric FAK inhibitor, with IC50 values in the low micromolar range.
    FAK inhibitor 5
  • HY-P10941
    VSLRGDTRG
    		Activator
    VSLRGDTRG is a synthetic peptide containing the RGD motif from cadherin 17 (CDH17), which binds to α2β1 integrin and activates its signaling pathway. VSLRGDTRG promotes the high-affinity conformational change of β1 integrin through the RGD motif, enhancing cell adhesion and phosphorylation of FAK and ERK1/2, thereby driving tumor proliferation and metastasis. VSLRGDTRG can be used in research on cancers expressing CDH17, such as colon cancer and pancreatic cancer.
    VSLRGDTRG
  • HY-N6257R
    Cafestol (Standard)
    		Inhibitor
    Cafestol (Standard) is the analytical standard of Cafestol. This product is intended for research and analytical applications. Cafestol is an orally active diterpenoid and an inhibitor of ERK2. Cafestol has elevated blood lipids, anti-inflammatory, anti-angiogenic and anti-diabetic activities. In addition, Cafestol induces tumor cell apoptosis and autophagy, which can be used in the study of cancer.
    Cafestol (Standard)
  • HY-117836
    FAK-IN-16
    		Inhibitor
    FAK-IN-16 (compound OXA-11) is an orally active, selective focal adhesion kinase (FAK) inhibitor with an IC50 of 1.2 pM. FAK-IN-16 inhibits FAK phosphorylation at pFAK[Y397] and pFAK[Y861]. FAK-IN-16 slows tumor growth and reduces tumor vascularity, invasion. FAK-IN-16 potentiates effects of Cisplatin (HY-17394) on tumor cell proliferation and apoptosis in vitro and anti-tumor actions in mice.
    FAK-IN-16
  • HY-P10323
    T7 Peptide
    		Inhibitor
    T7 peptide is an endothelial cell-specific inhibitor. T7 peptide interacts with αVβ3 integrin to inhibit the FAK, PI3-kinase, PKB/Akt, and mTOR signaling pathways in endothelial cells, ultimately suppressing protein synthesis and inducing apoptosis.
    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-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-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
Cat. No. Product Name / Synonyms Application Reactivity