SirReal2

SirReal2 is a potent, isotype-selective Sirt2 inhibitor with an IC₅₀ value of 140 nM and has very little effect on the activities of Sirt3-5. SirReal2 leads to tubulin hyperacetylation in HeLa cells and induces destabilization of the checkpoint protein BubR1. SirReal2 combined with VS-5584 (HY-16585) suppresses tumor growth and extends the survival rate of mice in tumor xenograft model. SirReal2 is is promising for research of cancer, inflammation and neurodegeneration^[1][2][3][4]. IC50 & Target:IC50: 140 nM (Sirt2)^[1] In Vitro:SirReal2 (1 μM, 24 h) combined with VS-5584 (1μM, 24 h) inhibits acute myeloid leukemia cell proliferation, increases the proportion of apoptotic cells and induces cell cycle arrest^[3].
In Vivo:SirReal2 (4 mg/kg, i.p., every 3 days for 28 days) combined with VS-5584 (4mg/kg, i.p., every 3 days for 28 days) leads to an extension of the survival time of mice and exhibits significant anti-tumor effects^[3].
SirReal2 (50 mg/kg, i.p., every 3 days for 19 days) inhibits the expression of SIRT2, resumes NK cell tumor infltration and suppresses melanoma progression in WT mice^[4].