709002-46-0

Sirtuins (SIRTs) represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs). SIRT2 deacetylates histone H4 and α-tubulin and functions as a regulator of cell cycle progression, a determinant of myelination, a modulator of autophagy, and a suppressor of brain inflammation. SirReal2 is an aminothiazole that acts as a SIRT-rearranging ligand to selectively inhibit SIRT2 (IC₅₀ = 140 nM). SirReal2 is >1,000-fold more potent at inhibiting the activity of SIRT2 than that of SIRT1 or SIRT3-6. This compound has been shown to be active in HeLa cells by significantly increasing α-tubulin acetylation.

SirReal2 is an aminothiazole that is a potent and selective Sirt2 inhibitor.

SIRT2: 140 nM (IC₅₀)

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[1] TOBIAS RUMPF. Selective Sirt2 inhibition by ligand-induced rearrangement of the active site.[J]. Nature Communications, 2015: 6263. DOI: 10.1038/ncomms7263