Mitoguazone

Mitoguazone is an inhibitor of S-adenosylmethionine decarboxylase (SAMDC) and diamine oxidase (DAO; IC₅₀s = 1 and 0.33 µM for the rat and porcine enzymes, respectively).¹ It inhibits viral DNA integration and replication in HIV-1-infected primary human macrophages when used at a concentration of 0.14 µM.² Mitoguazone (10 µM) decreases viability and induces mitochondrial swelling and cristae degradation in L1210 murine skin lymphocytic leukemia cells.³ It reduces the proliferation of seven melanoma cancer cell lines (IC₅₀s = 0.09-6.6 µM). In vivo, mitoguazone (50 mg/kg per day), in combination with a-difluoromethylornithine (DFMO; Item No. 16889), decreases tumor weight in a patient-derived xenograft (PDX) mouse model of differentiated papillary adenocarcinoma.⁴

WARNING This product is not for human or veterinary use.

1. 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).

2. Jin, X., McGrath, M.S., and Xu, H. Inhibition of HIV expression and integration in macrophages by methylglyoxal-bis-guanylhydrazone. J. Virol. 89(22), 11179-11186 (2015).

3. Mikles-Robertson, F., Dave, C., and Porter, C.W. Apparent autophagocytosis of mitochondria in L1210 leukemia cells treated in vitro with 4,4'-diacetyl-diphenylurea-bis(guanylhydrazone). Cancer Res. 40(4), 1054-1061 (1980).

4. Fujimoto, S., Igarashi, K., Shrestha, R.D., et al. Antitumor effects of two polyamine antimetabolites combined with mitomycin C on human stomach cancer cells xenotransplanted into nude mice. Int. J. Cancer 35(6), 821-825 (1985).