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-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-13692
    1α-Hydroxyvitamin D5
    		Inhibitor
    1α-Hydroxyvitamin D5 (CARD-024) is a vitamin D analog with extremely low hypercalcemic effects. 1α-Hydroxyvitamin D5 effectively attenuates the pro-fibrotic response of colonic myofibroblasts to TGFβ and high-stiffness substrates by inhibiting the expression of αSMA, the phosphorylation of FAK, and the gene expression of MLCK and ET-1, while activating the anti-inflammatory pathway of IL-1β/COX-2. 1α-Hydroxyvitamin D5 can be used in research related to intestinal fibrosis associated with Crohn's disease.
    1α-Hydroxyvitamin D5
  • 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-169319
    FAK-IN-21
    		Inhibitor
    FAK-IN-21 (compound 9) is a FAK inhibitor with the IC50 of 37.52 nM. FAK-IN-21 inhibits cell growth and the phosphorylation of FAK. FAK-IN-21 can be used for study of diffuse gastric cancer.
    FAK-IN-21
  • HY-175039
    FAK-IN-28
    		Inhibitor
    FAK-IN-28 is an orally active FAK inhibitor (IC50 = 0.4 nM). FAK-IN-28 exhibits dual antiproliferative and anti-metastatic properties. FAK-IN-28 triggers caspase-3-dependent apoptosis via ROS elevation. FAK-IN-28 inhibits tumor growth without causing weight loss or hepatotoxicity. FAK-IN-28 is useful in the study of FAK-driven malignancies, such as colon cancer, cervical cancer, triple-negative breast cancer, and melanoma.
    FAK-IN-28
  • HY-43760
    FAK ligand-5
    		Inhibitor
    FAK ligand-5 is a FAK ligand. FAK ligand-5 can be coupled with a linker to synthesize BI-4464 (HY-124625). FAK ligand-5 can be used as a target protein ligand for PROTAC development, specifically for designing PROTAC FAK degraders. FAK ligand-5 can be used in the synthesis of PROTAC FAK degrader 4 (HY-178467). FAK ligand-5 can be used in cancer research.
    FAK ligand-5
  • HY-183120
    EGFR T790M/FAK-IN-2
    		Inhibitor
    EGFR T790M/FAK-IN-2 is an orally active dual FAK and EGFRT790M kinase inhibitor, with an IC50 of 1.03 nM against FAK and an IC50 of 3.89 nM against EGFRT790M. EGFR T790M/FAK-IN-2 exerts antiproliferative effects in drug-resistant cancer cells overexpressing FAK, inducing apoptosis and cell cycle arrest. EGFR T790M/FAK-IN-2 exhibits antitumor activity in a pancreatic cancer xenograft mouse model. EGFR T790M/FAK-IN-2 can be used for the research of pancreatic cancer, breast cancer and non-small cell lung cancer.
    EGFR T790M/FAK-IN-2
  • HY-120339
    STK899704
    		Inhibitor
    STK899704 is a tubulin polymerization inhibitor. STK899704 exhibits broad-spectrum inhibitory activity against various cancer cell lines with IC50 values ​​ranging from 0.2 to 1.0 μM. STK899704 disrupts the mitotic spindle structure, inducing G2/M phase cell cycle arrest. STK899704 inhibits the migration ability of HT29 cells by downregulating the FAK-MEK-ERK signaling pathway, thereby suppressing the expression and activity of MMP-2 and MMP-9. STK899704 activates caspase-3/7/8/9, leading to PARP cleavage and inducing apoptosis. STK899704 induces cellular senescence through the p53 pathway. STK899704 can be used in research on skin cancer, lung cancer, colon cancer, and other cancers.
    STK899704
  • HY-136699
    Excisanin A
    		Inhibitor
    Excisanin A is a potent anticancer agent. Excisanin A inhibits cell proliferation, migration, adhesion and invasion. Excisanin A decreases the expression of MMP-2, MMP-9, p-FAK, p-Src, integrin β1 protein. Excisanin A has the potential for the research of breast cancer.
    Excisanin A
  • HY-12289S
    Defactinib-d6
    		Inhibitor
    Defactinib-d6 is a deuterium labeled Defactinib (HY-12289). Defactinib is a novel FAK inhibitor with potential antiangiogenic and antineoplastic activities.
    Defactinib-d<sub>6</sub>
  • HY-163709
    PROTAC FAK degrader 2
    		Degrader
    PROTAC FAK degrader 2 is an orally active PROTAC FAK degrader with a DC50 of 60.10 nM. PROTAC FAK degrader 2 forms a ternary complex with FAK and CRBN E3 ubiquitin ligase, driving proteasome-mediated degradation of total and phosphorylated FAK. PROTAC FAK degrader 2 inhibits phosphorylation of AKT and ERK, suppressing their downstream signaling pathways. PROTAC FAK degrader 2 reduces cancer cell viability, adhesion, migration, and invasion. PROTAC FAK degrader 2 exerts anti-tumor activity in HCT8/T tumor xenografts in mice. PROTAC FAK degrader 2 can be used for the research of breast cancer, colorectal cancer, lung cancer.
    PROTAC FAK degrader 2
  • HY-178142
    Multi-kinase-IN-7
    		Inhibitor
    Multi-kinase-IN-7 is a multikinase inhibitor with IC50s of 2.19, 2.95, 3.59 and 9.31 μM against EGFR, VEGFR2, TrKA and CDK2, respectively. Multi-kinase-IN-7 shows moderate and weaker activity against FAK, AKT1, GSK3β and CDK5 with IC50 values of 6.3, 9.2, 11.7 and 23.4 μM, respectively. Multi-kinase-IN-7 displays broad spectrum anti­proliferative potential against NCI cancer cell lines. Multi-kinase-IN-7 induces cell cycle arrest, apoptosis and necrosis. Multi-kinase-IN-7 Inhibitor can be used for the study of breast cancer.
    Multi-kinase-IN-7
  • HY-178969
    GZD-257
    		Inhibitor
    GZD-257 is a brain-penetrant, ATP-competitive FAK inhibitor (IC50 = 14.3 nM), performing 4.77-fold selectivity with FAK to Pyk2 (IC50 = 68.2 nM). GZD-257 can significantly induce apoptosis of U118MG cells and arrest the cell cycle at the G2/M phase. GZD-257 can be used for the study of Glioblastoma (GBM).
    GZD-257
  • HY-N1372AR
    Fangchinoline (Standard)
    		Inhibitor
    Fangchinoline (Standard) is the analytical standard of Fangchinoline. This product is intended for research and analytical applications. Fangchinoline is isolated from Stephania tetrandra with extensive biological activities, such as enhancing immunity, anti-inflammatory sterilization and anti-atherosclerosis. Fangchinoline, a novel HIV-1 inhibitor, inhibits HIV-1 replication by impairing gp160 proteolytic processing. Fangchinoline targets Focal adhesion kinase (FAK) and suppresses FAK-mediated signaling pathway in tumor cells which highly expressed FAK. Fangchinoline induces apoptosis and adaptive autophagy in bladder cancer.
    Fangchinoline (Standard)
  • HY-181487
    FAK activator-1
    		Activator
    FAK activator-1 is a FAK activator and mucosal healing inducer.FAK activator-1 increases FAK phosphorylation at Tyr-397, promoting FAK activation.FAK activator-1 promotes mucosal healing.FAK activator-1 can be used for the research of nsaid-associated gastrointestinal mucosal injury.
    FAK activator-1
  • 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-122860
    SKLB-C05
    SKLB-C05 is a novel selective, orally active TOPK inhibitor, with an IC50 of 0.5 nM. SKLB-C05 selectively inhibit TOPK kinase. SKLB-C05 induces Apoptosis, downregulates c-Myc, γ-H2AX, activates p53, blocks FAK/Src medicated migration-related signaling. SKLB-C05 disturbs cell mitosis. SKLB-C05 shows anticancer activity only against TOPK-positive colorectal cancer.
    SKLB-C05
  • HY-183768
    PROTAC FAK degrader 5
    		Inhibitor
    PROTAC FAK degrader 5 is a potent PROTAC degrader targeting FAK, with a DC50 of 11.65 nM. PROTAC FAK degrader 5 induces FAK protein degradation, selectively inhibits colony formation of human colorectal cancer HCT116 cells, and blocks the proliferation of human umbilical vein endothelial HUVEC cells, exhibiting anti-angiogenic activity. PROTAC FAK degrader 5 can be used in the research of colorectal cancer and angiogenesis.
    PROTAC FAK degrader 5
Cat. No. Product Name / Synonyms Application Reactivity