M 344 is an inhibitor of histone deacetylases (HDACs), inhibiting maize HDAC (IC50 = 100 nM)1 as well as human HDAC1 (IC50 = 46 nM).2 It shows a three-fold selectivity for inhibition of HDAC6 over HDAC1.3 M 344 enhances the sensitivity of human squamous carcinoma cells to radiation4 and promotes cell cycle arrest and apoptosis in human endometrial cancer and ovarian cancer cells (ED50 = 2.3 μM).5
1
Jung, M., Brosch, G., Kölle, D., et al. Amide analogues of trichostatin A as inhibitors of histone deacetylase and inducers of terminal cell differentiation. J Med Chem424669-4679(1999).
2
Remiszewski, S.W., Sambucetti, L.C., Atadja, P., et al. Inhibitors of human histone deacetylase: Synthesis and enzyme and cellular activity of straight chain hydroxamates. J Med Chem45(4)753-757(2002).
3
Heltweg, B., Dequiedt, F., Marshall, B.L., et al. Subtype selective substrates for histone deacetylases. J Med Chem475235-5243(2004).
4
Zhang, Y., Jung, M., Dritschilo, A., et al. Enhancement of radiation sensitivity of human squamous carcinoma cells by histone deacetylase inhibitors. Radiat Res161667-674(2004).
5
Takai, N., Ueda, T., Nishida, M., et al. M344 is a novel synthesized histone deacetylase inhibitor that induces growth inhibition, cell cycle arrest, and apoptosis in human endometrial cancer and ovarian cancer cells. Gynecol Oncol101108-113(2006).
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ONC(=O)CCCCCCNC(=O)c1ccc(cc1)N(C)C
Background Reading
Zhang, Y., Jung, M., Dritschilo, A., et al. Enhancement of radiation sensitivity of human squamous carcinoma cells by histone deacetylase inhibitors. Radiat Res161667-674(2004).
Jung, M., Brosch, G., Kölle, D., et al. Amide analogues of trichostatin A as inhibitors of histone deacetylase and inducers of terminal cell differentiation. J Med Chem424669-4679(1999).
Takai, N., Ueda, T., Nishida, M., et al. M344 is a novel synthesized histone deacetylase inhibitor that induces growth inhibition, cell cycle arrest, and apoptosis in human endometrial cancer and ovarian cancer cells. Gynecol Oncol101108-113(2006).
Heltweg, B., Dequiedt, F., Marshall, B.L., et al. Subtype selective substrates for histone deacetylases. J Med Chem475235-5243(2004).
Remiszewski, S.W., Sambucetti, L.C., Atadja, P., et al. Inhibitors of human histone deacetylase: Synthesis and enzyme and cellular activity of straight chain hydroxamates. J Med Chem45(4)753-757(2002).