Antipain is a protease inhibitor originally isolated from actinomycetes.[1] It inhibits thrombokinase, plasmin, trypsin, and papain in vitro (IC50s = 20, 93, 0.26, and 0.16 μg/ml, respectively). Antipain (6-600 μg/ml) inhibits the morphological transformation of and increases frequency of chromosomal aberrations in Syrian hamster embryo cells induced by N-methyl-N'-nitro-N-nitroso-guanidine (MNNG).[2] In vivo, antipain (25-100 mg/kg) suppresses urethan-induced formation of cleft palates and cleft lips in mice.[3]

Reference:

[1]. Suda, H., Aoyagi, T., Hamada, M., et al. Antipain, a new protease inhibitor isolated from actinomycetes. J. Antibiot. (Tokyo) 25(4), 263-266 (1972).

[2]. DiPaolo, J.A., Amsbaugh, S.C., and Popescu, N.C. Antipain inhibits N-methyl-N'-nitro-N-nitrosoguanidine-induced transformation and increases chromosomal aberrations. Proc. Natl. Acad. Sci. U.S.A. 77(11), 6649-6653 (1980).

[3]. Nomura, T., Enomoto, T., Shibata, K., et al. Antiteratogenic effects of tumor inhibitors, caffeine, antipain, and retinoic acid in mice. Cancer Res. 43(11), 5156-5162 (1983).

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