For research use only. Not for therapeutic Use.
FKGK18 is a selective group VIA calcium-independent phospholipase A2 (GVIA iPLA2) inhibitor. FKGK18 is a fluoroketone (FK)-based compound with IC50s of 50 nM and 3 μM for iPLA2β and iPLA2γ. FKGK18 can be used for the research of beta-cell apoptosis and diabetes[1][2][3].
FKGK18 (1 nM; 1 h) inhibits glucose-stimulated insulin secretion (GSIS) and prostaglandin E2 (PGE2) generation[2].
FKGK18 (0.1-10 nM; 24 h) inhibits beta-cell apoptosis[3].
FKGK18 (0.1-10 μM; 24 h) affects immune cells function and influences B-cell survival[3].
FKGK18 (20 mg/kg; i.p. three times per week from 10 days until euthanasia) reduces diabetes incidence[3].
| Catalog Number | I012637 |
| CAS Number | 1071001-09-6 |
| Synonyms | 1,1,1-trifluoro-6-naphthalen-2-ylhexan-2-one |
| Molecular Formula | C16H15F3O |
| Purity | ≥95% |
| InChI | InChI=1S/C16H15F3O/c17-16(18,19)15(20)8-4-1-5-12-9-10-13-6-2-3-7-14(13)11-12/h2-3,6-7,9-11H,1,4-5,8H2 |
| InChIKey | VCWWTQMRNJSJGC-UHFFFAOYSA-N |
| SMILES | C1=CC=C2C=C(C=CC2=C1)CCCCC(=O)C(F)(F)F |
| Reference | [1]. Kokotos G, et al. Potent and selective fluoroketone inhibitors of group VIA calcium-independent phospholipase A2. J Med Chem. 2010 May 13;53(9):3602-10. [2]. Ali T, et al. Characterization of FKGK18 as inhibitor of group VIA Ca2+-independent phospholipase A2 (iPLA2β): candidate drug for preventing beta-cell apoptosis and diabetes. PLoS One. 2013 Aug 20;8(8):e71748. [3]. Bone RN, et al. Inhibition of Ca2+-independent phospholipase A2β (iPLA2β) ameliorates islet infiltration and incidence of diabetes in NOD mice. Diabetes. 2015 Feb;64(2):541-54. |
