Home / Focal Adhesion Kinase Inhibitors / FAK Inhibitor 14

FAK Inhibitor 14

Catalog #: 3414
23 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
3414/10
3414/50
FAK Inhibitor 14 | CAS No. 4506-66-5 | Focal Adhesion Kinase Inhibitors
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Description: Selective FAK inhibitor
Alternative Names: Y15,NSC 677249

Chemical Name: 1,2,4,5-Benzenetetramine tetrahydrochloride

Product Details
Citations (23)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

FAK Inhibitor 14 is a selective focal adhesion kinase (FAK) inhibitor that displays no significant activity at a range of other kinases including EGFR, PDGFR and IGF-RI. FAK Inhibitor 14 prevents FAK autophosphorylation at Y397 (IC50 = 1 μM), promotes cell detachment and inhibits cell adhesion in vitro. FAK Inhibitor 14 exhibits antiproliferative activity in a variety of human tumor cell lines in vitro and in breast cancer cells in vivo.

Technical Data

M.Wt:
284.01
Formula:
C6H10N4.4HCl
Solubility:
Soluble to 50 mM in water and to 75 mM in DMSO
Storage:
Desiccate at RT
CAS No:
4506-66-5

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. CD146 mediates VEGF-induced melanoma cell extravasation through FAK activation.
    Jouve N, Bachelier R, Despoix N, Blin M, Matinzadeh M, Poitevin S, Aurrand-Lions M, Fallague K, Bardin N, Blot-Chabaud M, Vely F, Dignat-George F, Leroyer A
    Int J Cancer, 0;137(1):50-60.
  2. ORAI1 calcium channel orchestrates skin homeostasis.
    Vandenberghe M, Raphael M, Lehen'kyi V, Gordienko D, Hastie R, Oddos T, Rao A, Hogan P, Skryma R, Prevarskaya N
    Proc Natl Acad Sci U S A, 2013;110(50):E4839-48.
  3. The Src homology-2 protein Shb modulates focal adhesion kinase signaling in a BCR-ABL myeloproliferative disorder causing accelerated progression of disease.
    Gustafsson K, Jamalpour M, Trinh C, Kharas M, Welsh M
    J Hematol Oncol, 2014;7(0):45.
  4. Transmembrane collagen XVII modulates integrin dependent keratinocyte migration via PI3K/Rac1 signaling.
    Loffek S, Hurskainen T, Jackow J, Sigloch F, Schilling O, Tasanen K, Bruckner-Tuderman L, Franzke C
    PLoS ONE, 2014;9(2):e87263.
  5. Netrin-1 Preserves Blood-Brain Barrier Integrity Through Deleted in Colorectal Cancer/Focal Adhesion Kinase/RhoA Signaling Pathway Following Subarachnoid Hemorrhage in Rats
    Z Xie, B Enkhjargal, C Reis, L Huang, W Wan, J Tang, Y Cheng, JH Zhang
    J Am Heart Assoc, 2017;6(5):.
  6. Plectin protects podocytes from adriamycin-induced apoptosis and F-actin cytoskeletal disruption through the integrin ?6?4/FAK/p38 MAPK pathway
    Y Ni, X Wang, X Yin, Y Li, X Liu, H Wang, X Liu, J Zhang, H Gao, B Shi, S Zhao
    J. Cell. Mol. Med., 2018;0(0):.
  7. Involvement of TGFbeta-induced phosphorylation of the PTEN C-terminus on TGFbeta-induced acquisition of malignant phenotypes in lung cancer cells.
    Aoyama D, Hashimoto N, Sakamoto K, Kohnoh T, Kusunose M, Kimura M, Ogata R, Imaizumi K, Kawabe T, Hasegawa Y
    PLoS ONE, 2013;8(11):e81133.
  8. A small molecule inhibitor, 1,2,4,5-benzenetetraamine tetrahydrochloride, targeting the Y397 site of focal adhesion kinase decreases tumour growth.
    Golubovskaya et al.
    J.Med.Chem., 2008;51:7405
  9. A novel small molecule inhibitor of FAK decreases growth of human pancreatic cancer.
    Hochwald et al.
    Cell Cycle, 2009;8:2435

Product Datasheets

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Citations for FAK Inhibitor 14

The citations listed below are publications that use Tocris products. Selected citations for FAK Inhibitor 14 include:

23 Citations: Showing 1 - 10

  1. Focal adhesion kinase confers pro-migratory and antiapoptotic properties and is a potential therapeutic target in Ewing sarcoma.
    Authors: Konrad Et al.
    Mol Oncol  2020;14:248-260
  2. Vitronectin from brain pericytes promotes adult forebrain neurogenesis by stimulating CNTF.
    Authors: Theo Et al.
    Exp Neurol  2019;312:20-32
  3. Fibroblast activation protein-α promotes the growth and migration of lung cancer cells via the PI3K and sonic hedgehog pathways.
    Authors: Jia Et al.
    Int J Mol Med  2018;41:275
  4. Matrix stiffness modulates infection of endothelial cells by Listeria monocytogenes via expression of cell surface vimentin.
    Authors: Bastounis Et al.
    Mol Biol Cell  2018;29:1571
  5. Plectin protects podocytes from adriamycin-induced apoptosis and F-actin cytoskeletal disruption through the integrin α6β4/FAK/p38 MAPK pathway.
    Authors: Ni Et al.
    J Cell Mol Med  2018;22:5450
  6. Homodimers of vanillin and apocynin decrease the metastatic potential of human cancer cells by inhibiting the FAK/PI3K/Akt signaling pathway.
    Authors: Jantaree Et al.
    J.Agric.Food Chem.  2017;65:2299
  7. Netrin-1 suppresses the MEK/ERK pathway and ITGB4 in pancreatic cancer.
    Authors: An Et al.
    Oncotarget  2016;7:24719
  8. Integrin-FAK signaling rapidly and potently promotes mitochondrial function through STAT3.
    Authors: Visavadiya
    Cell Communication and Signaling  2016;14:32
  9. Endothelial Cells Use a Formin-Dependent Phagocytosis-Like Process to Internalize the Bacterium Listeria monocytogenes.
    Authors: Rengarajan Et al.
    PLoS One  2016;12:e1005603
  10. Inhibition of STAT3, FAK and Src mediated signaling reduces cancer stem cell load, tumorigenic potential and metastasis in breast cancer.
    Authors: Thakur Et al.
    Sci Rep  2015;5:10194
  11. Combination of heat shock protein 90 and focal adhesion kinase inhibitors synergistically inhibits the growth of non-small cell lung cancer cells.
    Authors: Webber Et al.
    Oncoscience  2015;2:765
  12. RECK-Mediated β1-Integrin Regulation by TGF-β1 Is Critical for Wound Contraction in Mice.
    Authors: Gutiérrez Et al.
    J Neurosci  2015;10:e0135005
  13. Palladin mediates stiffness-induced fibroblast activation in the tumor microenvironment.
    Authors: McLane and Ligon
    Biophys J  2015;109:249
  14. Astroglial-derived periostin promotes axonal regeneration after spinal cord injury.
    Authors: Shih Et al.
    Auton Neurosci  2014;34:2438
  15. OE and tamox. induce cell migration through GPR30 and activation of focal adhesion kinase (FAK) in endometrial cancers with low or without nuclear estrogen receptor α (ERα).
    Authors: Tsai Et al.
    PLoS One  2013;8:e72999
  16. ERBB4 confers metastatic capacity in Ewing sarcoma.
    Authors: Mendoza-Naranjo Et al.
    EMBO Mol Med  2013;5:1019
  17. Lysyl oxidase activity regulates oncogenic stress response and tumorigenesis.
    Authors: Wiel Et al.
    Cell Death Dis  2013;4:e855
  18. CB1 cannabinoid receptors couple to focal adhesion kinase to control Ins release.
    Authors: Malenczyk Et al.
    J Biol Chem  2013;288:32685
  19. Pathogenic NPHP5 mutations impair protein interaction with Cep290, a prerequisite for ciliogenesis.
    Authors: Barbelanne Et al.
    Hum Mol Genet  2013;22:2482
  20. Inhibition of a novel specific neuroglial integrin signaling pathway increases STAT3-mediated CNTF expression.
    Authors: Keasey Et al.
    Cell Commun Signal  2013;11:35
  21. Contractile equilibration of single cells to step changes in extracellular stiffness.
    Authors: Daniel A Et al.
    Biophys J  2012;102:443-51
  22. Inhibitors of Src and focal adhesion kinase promote endocrine specification: impact on the derivation of β-cells from human pluripotent stem cells.
    Authors: Afrikanova Et al.
    J Biol Chem  2011;286:36042
  23. GABAB receptor activation protects neurons from apoptosis via IGF-1 receptor transactivation.
    Authors: Tu Et al.
    J Neurosci  2010;30:749

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