| Bioactivity | 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]. | |||||||||
| Target | IC50: 50 nM (iPLA2β), 3 μM (iPLA2γ) | |||||||||
| Invitro | 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]. Cell Viability Assay[2] Cell Line: | |||||||||
| In Vivo | FKGK18 (20 mg/kg; i.p. three times per week from 10 days until euthanasia) reduces diabetes incidence[3]. Animal Model: | |||||||||
| Name | FKGK18 | |||||||||
| CAS | 1071001-09-6 | |||||||||
| Formula | C16H15F3O | |||||||||
| Molar Mass | 280.28 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| 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. |