You are here:Home-Inhibitors & Agonists-Tyrosine Kinase-c-Fes Kinase

Request The Product List ofc-Fes Kinase c-Fes Kinase

Tyrosine-protein kinase Fes/Fps (also known as proto-oncogene c-Fes/Fps) and together with the homologous kinase Fer, defines a structurally unique kinase family. c-Fes is present in a variety of cell lineages, including myeloid hematopoietic, vascular endothelial, neuronal and epithelial cells. Active c-Fes has been observed in acute myeloid leukemia (AML), and reduction of c-fes expression by RNAi demonstrated a requirement for c-Fes in AML cell survival.

Selective small molecule inhibitors are urgently needed to clarify the roles of c-Fes as dominant oncogene vs. tumor suppressor depending upon the cellular context. Despite the intriguing biology associated with c-Fes, very limited inhibitors with a useful level of selectivity and cellular activity have been reported to date.

TAE684, a compound previously identified as a potent and selective inhibitor of the anaplastic lymphoma kinase (ALK), is also a potent inhibitor of c-Fes both in vitro and in vivo. WZ-4-49-8 as well as HG-7-92-01 demonstrated strong inhibition of c-Fes in vitro. WZ-4-49-8 potently inhibited c-Fes-L145P-mediated soft-agar colony growth and showed remarkable selectivity for c-Fes-L145P over several active SFKs tested.

 

References:

1. Hellwig S, et al. Chem Biol. 2012 Apr 20;19(4):529-40.

2. Fei F, et al. BMC Biochem. 2010 Dec 1;11:48.

3. Olvedy M, et al. J Clin Invest. 2017 Jun 1;127(6):2310-2325.

4. Kanda S, et al. J Biol Chem. 2003 Mar 7;278(10):8244-9.

5. Stanicka J, et al. Oncogene. 2018 Jun;37(23):3131-3150.

 

Cat. No. Product Name CAS No. Information
PC-61640

HG-7-92-01

1315355-93-1

HG-7-92-01 is a potent, selective c-Fes protein-tyrosine kinase inhibitor with IC50 of 292 nM, displays intermediate selectivity profiles (selectivity score=0.18) against 353 kinases.

PC-61639

HG-7-27-01

1135270-45-9

HG-7-27-01 is a potent, selective c-Fes protein-tyrosine kinase inhibitor with IC50 of 224 nM, displays intermediate selectivity profiles (selectivity score=0.16) against 442 kinases.

PC-61638

WZ-4-49-8

1125594-27-5

WZ-4-49-8 is a potent, selective c-Fes protein-tyrosine kinase inhibitor with IC50 of 67 nM; displays an exceptional selectivity profile with a selectivity score of only 0.027 in a panel of 442 kinases; inhibits c-Fes-L145P autophosphorylation and microtubule association in at least a subset of cells, and potently inhibits c-Fes-L145P-mediated soft-agar colony growth; dramatically inhibits osteoclast differentiation in RAW 264.7 macrophage cell line.

Request The Product List

* Indicates a Required FieldYour information is safe with us.

  • *Product List:
  • *Applicant name:
  • *Email address:
  • *Organization name:
  • *Country:
  • Additional Information:
Contact Us sales@probechem.com