FKGK18 (FKGK-18) is a potent, selective inhibitor of iPLA2 (group VIA Ca2+-independent phospholipase A2) with IC50 of 50 nM.
FKGK18 displays 195 and >455 times more potent for GVIA iPLA(2) than for GIVA cPLA(2) and GV sPLA(2).
FKGK18 inhibits Ca2+-independent PLA2 activity in a concentration-dependent manner, similar to S-BEL, which preferentially inhibits cytosol-associated iPLA2β.
FKGK18 a valuable tool to explore the role of GVIA iPLA(2) in cells and in vivo models.
Physicochemical Properties
M.Wt
280.29
Formula
C16H15F3O
Appearance
Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
1,1,1-trifluoro-6-(naphthalen-2-yl)hexan-2-one
References
1. Kokotos G, et al. J Med Chem. 2010 May 13;53(9):3602-10.
2. Ali T, et al. PLoS One. 2013 Aug 20;8(8):e71748.
3. Bone RN, et al. Diabetes. 2015 Feb;64(2):541-54.
4. Dedaki C, et al. J Med Chem. 2019 Mar 12. doi: 10.1021/acs.jmedchem.8b01216.
