BML-278 is an activator of sirtuin 1 (SIRT1) that has an EC150 value (effective concentration able to increase the enzyme by 150%) of 1 uM. It less potently activates SIRT2 and SIRT3 (EC150s = 25 and 50 uM, respectively). BML-278 induces hypoacetylation on α-tubulin in U937 cells that are pretreated with SAHA , a histone deacetylase inhibitor. It arrests cell cycling at the G1/S phase, reduces senescence in primary human mesenchymal cells, and significantly increases mitochondrial density in murine C2C12 myoblasts.

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