Sardomozide is an inhibitor of S-adenosylmethionine decarboxylase (SAMDC), an enzyme involved in polyamine biosynthesis (IC50 = 0.005 ?M for the rat liver enzyme).1 It is selective for SAMDC over diamine oxidase (DAO; IC50 = 18 ?M for the rat small intestine enzyme). Sardomozide inhibits the proliferation of T24 bladder cancer cells (IC50 = 0.71 ?M). It decreases intracellular levels of spermidine and spermine and increases intracellular putrescine levels in L1210 murine leukemia cells when used at a concentration of 3 ?M.2 Sardomozide (0.2 and 0.4 ?M) inhibits HIV-1 replication in PM1 cells.3 It reduces tumor growth in a SK-MEL-24 melanoma mouse xenograft model when administered at doses of 0.5 and 5 mg/kg.2
1.Stanek, J., Caravatti, G., Frei, J., et al.4-Amidinoindan-1-one 2'-amidinohydrazone: A new potent and selective inhibitor of S-Adenosylmethionine decarboxylaseJ. Med. Chem.36(15)2168-2171(1993) 2.Regenass, U., Mett, H., Stanek, J., et al.CGP 48664, a new S-adenosylmethionine decarboxylase inhibitor with broad spectrum antiproliferative and antitumor activityCancer Res.54(12)3210-3217(1994) 3.Sch?fer, B., Hauber, I., Bunk, A., et al.Inhibition of multidrug-resistant HIV-1 by interference with cellular S-adenosylmethionine decarboxylase activityJ. Infect. Dis.194(6)740-750(2006)