SIRT3 Inhibitor

Sirt1/2-IN-1 (Compound 7) is a SIRT1 and SIRT2 inhibitor with IC₅₀ values of 1.81, 2.10 and 20.5 µg/mL against SIRT1, SIRT2 and SIRT3, respectively. Sirt1/2-IN-1 displays activity in hyperacetylation of α-tubulin protein with an IC₅₀ of 32.05 µg/mL. Sirt1/2-IN-1 shows prominent anticancer activity.

SIRT2-IN-14 (Compound 78) is a selectve inhibitor for SIRT2 with an IC₅₀ of 0.196 μM.

SIRT6-IN-4 (Compound 10d) is a selective inhibitor for SIRT6 with an IC₅₀ of 5.68 μM. SIRT6-IN-4 inhibits the proliferation of MCF-7 with an IC₅₀ of 8.30 μM. SIRT6-IN-4 arrests the cell cycle at G2/M phase, inhibits thecell migration and invasion of MCF-7, and induces apoptosis. SIRT6-IN-4 exhibits antitumor efficacy in mouse models.

SIRT3-IN-2 (Inhibitor scaffolds in Scheme 1) is a SIRT3 inhibitor, reducing SIRT3 activity by 39% at a concentration of 200 µM. SIRT3-IN-2 is promising for research into metabolic homeostasis and tumor suppression.

SIRT-IN-6 (Compound 14) is a pan-inhibitor of SIRT1/2/3 with IC₅₀ values of >50 μM. SIRT-IN-6 is promising for research of metabolic, inflammatory, oncologic and neurodegenerative disorders.