c-Fes Kinase (inhibitors, antagonists, agonists)-ProbeChem.com

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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	Information
PC-61640	HG-7-92-01 TAK1/MAP4K2 inhibitor, c-Fes inhibitor	HG-7-92-01 (NG25) is a potent, selective c-Fes protein-tyrosine kinase inhibitor with IC50 of 292 nM, also is a potent dual TAK1 and MAP4K2 inhibitor, with IC50s of 149 nM and 21.7 nM, respectively.
PC-61639	HG-7-27-01 c-Fes inhibitor	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 c-Fes inhibitor	WZ-4-49-8 is a potent, selective c-Fes protein-tyrosine kinase inhibitor with IC50 of 67 nM.

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