Sardomozide (hydrochloride)

Sardomozide is an inhibitor of S-adenosylmethionine decarboxylase (SAMDC), an enzyme involved in polyamine biosynthesis (IC₅₀ = 0.005 µM for the rat liver enzyme).¹ It is selective for SAMDC over diamine oxidase (DAO; IC₅₀ = 18 µM for the rat small intestine enzyme). Sardomozide inhibits the proliferation of T24 bladder cancer cells (IC₅₀ = 0.71 µM). 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 µM.² Sardomozide (0.2 and 0.4 µM) 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

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1. Stanek, J., Caravatti, G., Frei, J., et al. 4-Amidinoindan-1-one 2'-amidinohydrazone: A new potent and selective inhibitor of S-Adenosylmethionine decarboxylase. J. 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 activity. Cancer Res. 54(12), 3210-3217 (1994).

3. Schäfer, B., Hauber, I., Bunk, A., et al. Inhibition of multidrug-resistant HIV-1 by interference with cellular S-adenosylmethionine decarboxylase activity. J. Infect. Dis. 194(6), 740-750 (2006).