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-15323
    PRT062607 Hydrochloride
    		Inhibitor 98.07%
    PRT062607 (P505-15) Hydrochloride is an orally available Syk inhibitor (IC50: 1 nM) that inhibits inflammation and induction Apoptosis. PRT062607 Hydrochloride exerts potent antitumor activity in tumor xenograft mouse models.
    PRT062607 Hydrochloride
  • HY-109582
    ADT-OH
    		98.55%
    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
  • HY-13203
    NVP-TAE 226
    		Inhibitor 99.77%
    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
  • HY-139344
    FC-11
    		Degrader 99.95%
    FC-11 is a PROTAC FAK degrader (DC90: 1 nM) . FC-11 contains CRBN ligand Pomalidomide (HY-10984), linker and FAK ligand PF562271 (HY-10459).
    FC-11
  • HY-16468
    Squalamine
    		Inhibitor 99.54%
    Squalamine (MSI-1256) is an aminosterol compound with broad-spectrum antiviral activity. Squalamine makes cells less conducive to certain viral replication by altering the electrostatic interactions in the inner membrane of host cells. Squalamine also has antibacterial and antitumor activities. Squalamine has broad-spectrum antibacterial activity against Gram-negative and Gram-positive bacteria, fungi and protozoa. Squalamine inhibits tumor-related angiogenesis and the growth of human breast cancer cells. Squalamine restores the function of enteric nervous system in Parkinson,s disease mouse models.
    Squalamine
  • HY-15841
    CEP-37440
    		Inhibitor 99.91%
    CEP-37440 is a potent, orally active dual FAK/ALK inhibitor with IC50 values of 2.3 nM and 3.5 nM for FAK and ALK, respectively. CEP-37440 decreases the cell proliferation by blocking the autophosphorylation kinase activity of FAK1 (Tyr 397).
    CEP-37440
  • HY-13917A
    PND-1186 hydrochloride
    		Inhibitor 99.92%
    PND-1186 hydrochloride (VS-4718 hydrochloride) is a potent, highly-specific and reversible inhibitor of FAK with an IC50 of 1.5 nM. PND-1186 hydrochloride selectively promotes tumor cell apoptosis.
    PND-1186 hydrochloride
  • HY-119932
    PROTAC FAK degrader 1
    		Inhibitor 99.25%
    PROTAC FAK degrader 1 (Compound PROTAC-3) is a selective and effective degrader of Fak PROTAC with a DC50 of 3.0 nM. PROTAC FAK degrader 1 reduces the ability of cancer cells to migrate and invade. PROTAC FAK degrader 1 can be used in the study of tumor. (Pink: Fak ligand (HY-44146); Black: Linker (HY-44141); Blue: VHL ligand 1 (HY-125845)).
    PROTAC FAK degrader 1
  • HY-N6257
    Cafestol
    		Inhibitor 99.91%
    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
  • HY-158231
    Polyether F127 Diacrylate
    		Activator
    Polyether F127 Diacrylate (F127DA) is an acrylated polyethylene glycol-polypropylene glycol-polyethylene glycol triblock copolymer. Polyether F127 Diacrylate rapidly crosslinks and cures into a gel under ultraviolet or visible light with the action of a photoinitiator. Polyether F127 Diacrylate exhibits excellent thermogelation properties and favorable biosafety. Polyether F127 Diacrylate can upregulate the Integrin-FAK pathway, enhance collagen production, increase the protein and gene expression levels of COL-1/SCX, and promote fibroblastic differentiation of periodontal ligament stem cells. Polyether F127 Diacrylate promotes periodontal ligament regeneration and reduces abnormal healing in a rat model of delayed replanted teeth. Polyether F127 Diacrylate promotes functional osteochondral regeneration in a rat model of osteoarthritis. Polyether F127 Diacrylate supports adipose tissue survival, rendering it suitable for breast reconstruction applications. Polyether F127 Diacrylate can be used in studies related to periodontal ligament injury, breast defect and osteoarthritis.
    Polyether F127 Diacrylate
  • HY-105935
    Keracyanin chloride
    		Inhibitor 99.90%
    Keracyanin chloride inhibits NF-κB/FAK/MAPK signaling pathway. Keracyanin chloride exhibits antioxidant, anti-inflammatory and hypoglycemic effects, and is orally active.
    Keracyanin chloride
  • HY-111546
    BI-3663
    		Inhibitor 99.84%
    BI-3663 is a highly selective PTK2/FAK PROTAC (DC50=30 nM), with Cereblon ligands to hijack E3 ligases for PTK2 degradation. BI-3663 inhibits PTK2 with an IC50 of 18 nM. BI-3663 is a PROTAC that composes of BI-4464 (HY-124625) linked to Pomalidomide (HY-10984) with a linker. Anti-cancer activity.
    BI-3663
  • HY-148385
    Ganglioside GM2
    		Activator 98.0%
    Ganglioside GM2 is a human tumor antigen predominantly found in human tumor cells and fetal brain tissue. As a sialylated glycosphingolipid, Ganglioside GM2 is involved in processes such as cell signaling, adhesion, and motility. Ganglioside GM2 abnormal expression and accumulation are associated with tumors and neurodegenerative disorders. Ganglioside GM2 promotes tumor cell migration and invasion by directly binding to the integrin β1 receptor, activating the FAK/Src/Erk-MAPK signaling pathway, and inducing actin cytoskeleton remodeling.
    Ganglioside GM2
  • HY-109084
    Conteltinib
    		Inhibitor 99.0%
    Conteltinib (CT-707) is a multi-kinase inhibitor targeting FAK, ALK, and Pyk2. Conteltinib exerts significant inhibitory effect on FAK with an IC50 of 1.6 nM.
    Conteltinib
  • HY-105174A
    BPC 157 acetate
    		Activator 99.78%
    BPC 157 acetate is an orally active peptide. BPC 157 acetate exhibits multiple activities such as promoting wound healing, tendon healing, neuroprotection, and gastrointestinal protection. BPC 157 acetate can be used in the research of tendon injury, burn, gastric ulcer, and neurological diseases.
    BPC 157 acetate
  • HY-120417
    JP-153
    		Inhibitor 99.45%
    JP-153 is the Src-FAK-Paxillin signaling inhibitor. JP-153 inhibits Src-dependent phosphorylation of paxillin (Y118) and downstream activation of Akt (S473). JP-153 reduces VEGF-induced migration and proliferation in retinal endothelial cells. JP-153 can be uesd for the study of neovascular eye disease.
    JP-153
  • HY-148877
    AT-533
    		Inhibitor 98.38%
    AT-533 is a potent Hsp90 and HSV inhibitor. AT-533 suppresses tumor growth and angiogenesis by blocking the HIF-1α/VEGF/VEGFR-2 signaling pathway. AT-533 also inhibits the activation of the downstream pathways, including Akt/mTOR/p70S6K, Erk1/2 and FAK. AT-533 inhibits the tube formation, cell migration, and invasion of human umbilical vein endothelial cells (HUVECs).
    AT-533
  • HY-P10941A
    VSLRGDTRG acetate
    		Activator 99.38%
    VSLRGDTRG acetate is a synthetic peptide containing the RGD motif from cadherin 17 (CDH17), which binds to α2β1 integrin and activates its signaling pathway. VSLRGDTRG acetate 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 acetate can be used in research on cancers expressing CDH17, such as colon cancer and pancreatic cancer.
    VSLRGDTRG acetate
  • HY-171770
    dAurAB5
    		99.03%
    dAurAB5 is a dual Aurora-A (DC50 = 8.8 nM) and Aurora-B (DC50 = 6.1 nM) PROTAC degrader. dAurAB5 induces degradation of Aurora-A and Aurora-B, reduces N-Myc levels, and decreases viability in IMR32 neuroblastoma cells. dAurAB5 downregulates the levels of AAK1, PTK2, GAK, and TTK. dAurAB5 can be used to study cancers such as neuroblastoma. (Pink: TTK ligand 2: HY-168542, Blue: Thalidomide-O-COOH: HY-103597, Black: 6-Aminocaproic acid: HY-B0236).
    dAurAB5
  • HY-124625
    BI-4464
    		Inhibitor 98.64%
    BI-4464 is a highly selective, ATP competitive PTK2/FAK protein kinase inhibitor with an IC50 value of 17 nM. BI-4464 is a FAK (HY-43760) ligand and linker conjugate. BI-4464 can be used to construct proteolysis targeting chimeras (PROTACs), such as PROTAC FAK degrader 4 (HY-178467). PROTAC FAK degrader 4 is a highly potent and selective FAK PROTAC degrader.
    BI-4464
Cat. No. Product Name / Synonyms Application Reactivity