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-179679
    FAK-IN-29
    		Inhibitor
    FAK-IN-29 is a selective FAK inhibitor with an IC50 of 0.5 nM. FAK-IN-29 can inhibit the proliferation and colony formation of MDA-MB-231 cells, and induce cell cycle arrest and apoptosis. FAK-IN-29 exhibits antitumor activity and can be used for the research of tumors such as triple-negative breast cancer.
    FAK-IN-29
  • 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-181061
    COX/5-LO-IN-2
    		Inhibitor
    COX/5-LO-IN-2 is a COX2, EGFR, COX1, 5-LOX, BRAF and FAK inhibitor with IC50 of 1.22 μM, 2.5 μM, 2.95 μM, 4.65 μM, 7.4 μM, 12.2 μM, respectively. COX/5-LO-IN-2 induces cell growth arrest at G2/M phase. COX/5-LO-IN-2 triggers apoptotic activity by up-regulating proapoptotic proteins p53, Bax, and caspase-7 and down-regulating anti-apoptotic protein Bcl-2. COX/5-LO-IN-2 can be used for the research of breast cancer.
    COX/5-LO-IN-2
  • 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-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-W040971S
    Creosol-d4
    		Inhibitor
    Creosol-d4 (2-Methoxy-4-methylphenol-d4) is the deuterium labeled Creosol (HY-W040971). 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-d<sub>4</sub>
  • 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-181732
    PROTAC TG2 Degrader-3
    		Modulator
    PROTAC TG2 Degrader-3 is a TG2 (TGM2) PROTAC degrader. PROTAC TG2 Degrader-3 inhibits the adhesion and migration of ovarian cancer cells. PROTAC TG2 Degrader-3 can be used for the research of ovarian cancer.
    PROTAC TG2 Degrader-3
  • 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-138082
    Rac-ZINC4085554
    Rac-ZINC4085554 is the racemic form of ZINC4085554. ZINC4085554 interferes with the interaction between Akt1 and FAK. ZINC4085554 is useful in colon cancer research.
    Rac-ZINC4085554
  • HY-183769
    FAK-IN-31
    		Inhibitor
    FAK-IN-31 is a FAK inhibitor with antiproliferative activity against a variety of cancer cell lines. FAK-IN-31 serves as a PROTAC target protein ligand for the development of FAK-targeted PROTAC degrader heads, such as PROTAC FAK degrader 5 (HY-183768). FAK-IN-31 can be used in the research of colorectal cancer, pancreatic cancer, breast cancer, hepatocellular carcinoma and lung cancer.
    FAK-IN-31
  • 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-138195
    NEO212
    		Inhibitor
    NEO212 is an orally active, blood-brain barrier permeable conjugate of Temozolomide (TMZ) (HY-17364) and Perillyl Alcohol (POH) (HY-N7000), with potent anticancer activity. NEO212 overcomes classical TMZ resistance and DNA alkylation by depleting MGMT. By inhibiting the FAK/Src signaling pathway, NEO212 reduces the production of MMP2 and MMP9, induces mesenchymal-epithelial transition, and inhibits the migration, invasion and tumor progression of glioma stem cells. NEO212 disrupts autophagy flux to enhance mitochondrial apoptosis; it induces differentiation of acute myeloid leukemia (AML) cells into macrophages and proliferation arrest.
    NEO212
  • 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-176198
    BI-0319
    		Degrader
    BI-0319 is a selective PTK2/FAK PROTAC degrader. BI-0319 can reduce cancer cells viability inhibit proliferation and invasion. BI-0319 can be used for the research of cancer, such as liver cancer. (Structure Note: Pink: PTK2/FAK ligand (HY-43760); Blue: VHL ligand (HY-125845); Black: linker (HY-140189); VHL ligand-Linker: (HY-103602A))
    BI-0319
  • 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
Cat. No. Product Name / Synonyms Application Reactivity