HPA-12 is a ceramide analog and inhibitor of ceramide transfer protein (CERT). It inhibits binding of a ceramide probe to the isolated steroidogenic acute regulatory protein-related lipid transfer (START) domain of CERT with an EC50 value of 4 μM in a TR-FRET assay. HPA-12 (2.5 μM) inhibits conversion of the fluorescent ceramide analog C5-DMB-Cer to C5-DMB-sphingomyelin in CHO and HeLa cells. It also inhibits sphingomyelin synthesis in wild-type, but not ATP-dependent ceramide transport-deficient, CHO cells when used at a concentration of 1 μM.