MC2494 pan SIRT inhibitor (RGCNY-0118)
Per 10 mg
MC249 is a pan Sirtuin (SIRT) inhibitor. MC249 displays tumor-selective effects in vitro, in leukemic blasts ex vivo and in xenograft and allograft cancer models in vivo. MC249 was shown to induce tumor-restricted acetylated RIP1/caspase-8-mediated apoptosis and inhibits tumor cell migration. Importantly, MC249 has tumor-preventative activity by blocking 7,12-dimethylbenz(a)anthracene-induced mammary gland hyperproliferation in vivo. MC249 is a promising candidate for cancer treatment and prevention.
Systematic Name: (E)-3-(4-(2-chlorobenzoyl)-1H-pyrrol-2-yl)-2-cyano-N-(quinolin-5-yl)acrylamide
Mol Wt: 426.86
Carafa, V. et al. RIP1-HAT1-SIRT Complex Identification and Targeting in Treatment and Prevention of
Cancer. Clin. Cancer Res. 2018, 24, 2886–2900
Carafa, V. et al. Enzymatic and Biological Characterization of Novel Sirtuin Modulators against Cancer. Int. J. Mol. Sci. 2019, 20, 5654; doi:10.3390/ijms20225654.
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