FAK Inhibitor 14

Cat. No. 3414

FAK Inhibitor 14 C6H10N4.4HCl [4506-66-5]

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Alternative Names: Y15, NSC 677249

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

Biological Activity

Selective focal adhesion kinase (FAK) inhibitor that displays no significant activity at a range of other kinases including EGFR, PDGFR and IGF-RI. Prevents FAK autophosphorylation at Y397 (IC50 = 1 μM), promotes cell detachment and inhibits cell adhesion in vitro. 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.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Hochwald et al (2009) A novel small molecule inhibitor of FAK decreases growth of human pancreatic cancer. Cell Cycle 8 2435. PMID: 19571674.

Golubovskaya et al (2008) A small molecule inhibitor, 1,2,4,5-benzenetetraamine tetrahydrochloride, targeting the Y397 site of focal adhesion kinase decreases tumour growth. J.Med.Chem. 51 7405. PMID: 18989950.

If you know of a relevant reference for FAK Inhibitor 14 please let us know.

Citations are publications that use Tocris products. Selected citations for FAK Inhibitor 14 include:

Rengarajan et al (2016) Endothelial Cells Use a Formin-Dependent Phagocytosis-Like Process to Internalize the Bacterium Listeria monocytogenes. PLoS One 12 e1005603. PMID: 27152864.

Gutiérrez et al (2015) RECK-Mediated β1-Integrin Regulation by TGF-β1 Is Critical for Wound Contraction in Mice. J Neurosci 10 e0135005. PMID: 26247610.

Webber et al (2015) Combination of heat shock protein 90 and focal adhesion kinase inhibitors synergistically inhibits the growth of non-small cell lung cancer cells. Oncoscience 2 765. PMID: 26501082.

Shih et al (2014) Astroglial-derived periostin promotes axonal regeneration after spinal cord injury. Auton Neurosci 34 2438. PMID: 24523534.

Keasey et al (2013) Inhibition of a novel specific neuroglial integrin signaling pathway increases STAT3-mediated CNTF expression. Cell Commun Signal 11 35. PMID: 23693126.

Malenczyk et al (2013) CB1 cannabinoid receptors couple to focal adhesion kinase to control insulin release. J Biol Chem 288 32685. PMID: 24089517.

Mendoza-Naranjo et al (2013) ERBB4 confers metastatic capacity in Ewing sarcoma. EMBO Mol Med 5 1019. PMID: 23681745.

Wiel et al (2013) Lysyl oxidase activity regulates oncogenic stress response and tumorigenesis. Cell Death Dis 4 e855. PMID: 24113189.

Afrikanova et al (2011) Inhibitors of Src and focal adhesion kinase promote endocrine specification: impact on the derivation of β-cells from human pluripotent stem cells. J Biol Chem 286 36042. PMID: 21852242.

Tu et al (2010) GABAB receptor activation protects neurons from apoptosis via IGF-1 receptor transactivation. J Neurosci 30 749. PMID: 20071540.

Do you know of a great paper that uses FAK Inhibitor 14 from Tocris? If so please let us know.show all ▼show less ▲

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Keywords: FAK Inhibitor 14, supplier, Selective, FAK, inhibitors, inhibits, Focal, Adhesion, Kinases, Inhibitor14, Tocris Bioscience, Focal Adhesion Kinase Inhibitor products

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