SIRT2 Inhibitor

NCO-141 is a selective SIRT2 inhibitor with an IC₅₀ of 0.5 μM. NCO-141 induces cell apoptosis via caspase activation and mitochondrial superoxide anion production. NCO-141 induces cell autophagy by increasing LC3-II levels and autophagosome accumulation. NCO-141 is applicable to relevant research on leukemia.

Sirt2-IN-6 (compound 24a) potent and selective inhibitor of SIRT2, with an IC₅₀ of 0.815 μM. Sirt2-IN-6 can be used for the research of cancer.

Nicotinamide hydrochloride is a form of vitamin B3 or niacin. Nicotinamide hydrochloride inhibits SIRT2 activity (IC₅₀: 2 μM). Nicotinamide hydrochloride also inhibits SIRT1. Nicotinamide hydrochloride increases cellular NAD₊, ATP, ROS levels. Nicotinamide hydrochloride inhibits tumor growth and improves survival. Nicotinamide hydrochloride also has anti-HBV activity.

hsa62 is a dual inhibitor for SIRT1 and SIRT2, with IC₅₀ of 1.3 and 5.5 μM, respectively.

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.

Sirtuin-IN-1 (Compound 18) is a SIRT1/2 inhibitor (IC₅₀s: 6.2 μM and 4.2μM for SIRT1 and SIRT2, respectively). Sirtuin-IN-1 induces G1 cell cycle arrest. Sirtuin-IN-1 exhibits potent anti-cancer activity against glioma.

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

NCO-90 is a selective SIRT2 inhibitor with an IC₅₀ of 1.0 μM. NCO-90 induces Apoptosis via Caspase activation and mitochondrial superoxide anion production, and also induces Autophagic cell death by increasing LC3-II levels and autophagosome accumulation. NCO-90 exhibits anticancer activity against leukemia. NCO-90 can be used in research related to acute lymphoblastic leukemia and acute myeloid leukemia.

SL010110 is an anti-hyperglycemic agent. SL010110 potently inhibits gluconeogenesis by inhibiting SIRT2, activating p300, and subsequently promoting PEPCK1 degradation. SL010110 downregulates the protein level of PEPCK1 without affecting the gene expressions of PEPCK, glucose-6-phosphatase, and fructose-1,6-bisphosphatase. SL010110 significantly improves glucose homeostasis in type 2 diabetic (T2D) mice model. SL010110 can be used for T2D research.

SR94, a SR17 derivative, is a SIRT2 inhibitor that contains an arbitrary 6-member ring and different R2 groups. SR94 is promising for research of cancer, ischemia-reperfusion and neurodegenerative diseases.

HSP70/SIRT2-IN-1 (Compounds 2a) is a dual inhibitor for SIRT2 and HSP70, with IC₅₀ of 17.3±2.0 μM for SIRT2. HSP70/SIRT2-IN-1 has antitumor activity.

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.

A2B57 is a selective inhibitor for SIRT 2 with an IC₅₀ of 6.3 µM.

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.

SIRT2-IN-18 (Compound 8) is a SIRT2 inhibitor with IC₅₀s of 5.3  and 12.3 μM for SmSIRT2 and hSIRT2, respectively. SIRT2-IN-18 shows potent antischistosomal activities against both Liberian and Puerto Rican strains of Schistosoma mansoni and reduces schistosomula and adult worm pair viability, pairing, and egg production, with low cytotoxicity in mammalian cells. SIRT2-IN-18 increases histone H3 hyperacetylation and induces cytochrome c-mediated apoptosis.

A1B11 is a selective SIRT inhibitor (SIRT2:IC50=5.3 μM) that can be used in the study of neurodegenerative diseases.