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N¹-Acetylspermine is a monoacetylated derivative of spermine , an endogenous polyamine synthesized from spermidine , that displays lower K_m and higher V_max values than spermine, making it a better substrate of polyamine oxidase than the non-acetylated polyamine. Spermine is required for eukaryotic cell growth and protein synthesis and is involved in the modulation of calcium-dependent immune processes. N¹-Acetylspermine has been used to study the uptake of the anticancer polyamine analog bleomycin-A5 by the human carnitine transporter SLC22A16.

N1-Acetylspermine trihydrochloride has been used in a study to determine that the human carnitine transporter SLC22A16 mediates high affinity uptake of the anticancer polyamine analogue bleomycin-A5.