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C2 L-threo Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides.¹ It stimulates cholesterol efflux in CHO cells expressing the human ABCA1 receptor when used at a concentration of 10 μM, however, this efflux is 50% less than that stimulated by C2 ceramide . C2 L-threo Ceramide inhibits IL-4 production by 17% in EL4 T cells stimulated with phorbol 12-myristate 13-acetate (PMA; ) when used at a concentration of 10 μM.² It also induces cell cycle arrest in the G₀/G₁ phase and a 7-fold increase in sphingosine accumulation as well as inhibits growth of HL-60 leukemia cells.^3,4

1. Ghering, A.B., and Davidson, W.S. Ceramide structural features required to stimulate ABCA1-mediated cholesterol efflux to apolipoprotein A-I J. Lipid Res. 47(12),2781-2788(2006).
2. Park, J., Li, Q., Chang, Y.T., et al. Inhibitory activity of a ceramide library in interleukin-4 production from activated T cells Bioorg. Med. Chem. 13(7),2589-2595(2005).
3. Baek, M.Y., Yoo, H.S., Nakaya, K., et al. Sphingolipid metabolic changes during chiral C₂-ceramides induced apoptosis in human leukemia cells Arch. Pharm. Res. 24(2),144-149(2001).
4. Bielawska, A., Crane, H.M., Liotta, D., et al. Selectivity of ceramide-mediated biology. Lack of activity of erythro-dihydroceramide J. Biol. Chem. 268(35),26226-26232(1993).