F-12509A Cyclic Product K1 Yellow powder. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable tetracyclic quinone compound that acts as a specific, reversible, and non-competitive inhibitor of CerK (ceramide kinase) activity (IC50 ~5 µM) with little effect against SPHK1/2 or DGKg (IC50 >100 µM). Shown to reduce cellular C1P (ceramide-1-phosphate) synthesis by 40% at ≥20 µM in a rat basophilic leukemia cell line RBL-2H3 and block CerK-mediated degranulation in both RBL-2H3 and murine BMMC (bone marrow-derived mast cells) in a dose-dependent manner. Exhibits no cytotoxic effect against RBL-2H3 even at concentrations as high as 100 µM. Purity: ≥95% by NMR (mixture of enantiomers). Ref.: Kim, J.W., et al. 2007. Biochim. Biophys. Acta 1771, 1262. Kumada, H., et al. 2007. Biosci. Biotechnol. Biochem. 71, 2581 Kim, J.W., et al. 2005. Biochim. Biophys. Acta 1738, 82. Sold for research purposes only, pursuant to an agreement with Merck Japan. |