SIRTINOL

Sirtinol (410536-97-9) is an inhibitor of sirtuin family enzymes including human SIRT1 (IC50=60 μM), human SIRT2 (IC50=58 μM), and yeast Sir2 (IC50=48 μM) with no inhibition of human HDAC1. Active in vivo and in purified enzyme studies. Cell permeable.

Sirtinol is a cell permeable specific inhibitor of sirtuin NAD-dependant deacetylases

Sirtinol is a known inhibitor of the NAD+-Dependent Protein Desuccinylase and Demalonylase Sirt5 and exhibits anticancer properties.

ChEBI: Sirtinol is a benzamide obtained by formal condensation of the carboxy group of 2-{[(2-hydroxy-1-naphthyl)methylene]amino}benzoic acid with the amino group of 1-phenylethylamine. It has a role as an anti-inflammatory agent, an EC 3.5.1.98 (histone deacetylase) inhibitor and a Sir2 inhibitor. It is a member of benzamides, an aldimine and a member of naphthols. It is functionally related to an anthranilic acid.

A cell-permeable 2-hydroxy-1-naphthaldehyde derivative that acts as a specific and direct inhibitor of the sirtuin class of deacetylase activity with no affect on human HDAC1 (IC₅₀ = 48 μM, 131 μM and 58 μM for ySir2, hSIRT1 and hSIRT2, respectively). Reported to inhibit Sir2p transcriptional silencing activity in vivo (IC₅₀ = 25 μM), and NAD-dependent histone deacetylase activity of purified recombinant yeast Sir2p and human SIRT2 in vitro (IC₅₀ = 70 μM and 40 μM, respectively). A 10 mM (1 mg/254 μl) solution of Sirtinol (Cat. No. 566321) in DMSO is also available.

Cell-permeable, selective sirtuin deacetylase inhibitor (IC 50 values are 38, 68 and 131 μ M at SIRT2, Sir2p and SIRT1 respectively) that has no effect on HDAC1 activity. Significantly decreases growth and viability of PCa and HEK293T cells in vitro .

Cell permeable: yes

Store at -20°C

Sirtinol is a cell-permeable inhibitor of sirtuin NAD+-dependent histone deacetylases. It inhibits yeast sirtuin Sir2p with an IC50 value of 68 μM, and inhibits human SIRT1 and SIRT2 with IC50 values of 131 μM and 38 μM, respectively. Sirtinol does not inhibit human HDAC1 activity. It elevates endogenous levels of reactive oxygen species to induce apoptosis in cancer cells. Sirtinol inhibits proliferation of non-small cell lung cancer cells and suppresses inflammatory activity in human dermal microvascular endothelial cells. Sirtinol also activates the auxin signaling transduction pathway in Arabidopsis, altering plant growth and development.

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