sirt-2-in-1

Sirt2-IN-1 is an inhibitor of sirtuin 2 (IC50 = 163 nM).

SIRT2-IN-16 (compound 17) is a SIRT2 inhibitor targeted at prostate-specific membrane antigen (PSMA).

SIRT2-IN-17 (compound Z18) is a potent inhibitor of SIRT2, effectively reducing the expression of α-SMA and p-Smad2/3.

SIRT2-IN-12 (Compound 3) is a SIRT2 inhibitor with an IC50 value of 50 μM.

SIRT2-IN-18 (Compound 8) is a potent SIRT2 inhibitor, with IC50 values of 5.3 μM for SmSIRT2 and 12.3 μM for hSIRT2. It demonstrates strong anti-schistosomal activity against Schistosoma mansoni strains from Liberia and Puerto Rico, effectively reducing larval and adult worm pair survival, pairing, and egg production, while exhibiting low cytotoxicity to mammalian cells. Additionally, SIRT2-IN-18 enhances histone H3 hyperacetylation and induces apoptosis through cytochrome c mediation.

SIRT2-IN-10 (Compound 12) is a potent SIRT2 inhibitor (IC50: 1.3 μM) useful for cancer and neurodegenerative disease research.

SIRT2-IN-11 is a potent and selective SIRT2 inhibitor (IC50 = 12 nM). It increases tubulin acetylation without affecting SIRT1/3, used for studying SIRT2 function in cancer and neuroprotection.

HSP70/SIRT2-IN-1 (Compound 2a) serves as a dual inhibitor targeting both SIRT2 and HSP70, exhibiting an IC50 of 17.3±2.0 μM against SIRT2. This compound possesses antitumor activity [1].

**SIRT2-IN-14 (Compound 78)** is a selective SIRT2 inhibitor, demonstrating an IC50 value of 0.196 μM [1].

SIRT2-IN-15 (compound 1) acts as both a deacetylase and deglycosylase inhibitor for SIRT2, exhibiting IC50 values of 7 μM and 37 μM, respectively.

SIRT2-IN-13 (compound 7c) acts as an inhibitor of SIRT2, inducing apoptosis in cells. It selectively inhibits colon cancer and leukemia cells, causing a cell cycle arrest at the G2 phase.

SIRT-IN-1 is a potent inhibitor of SIRT1, SIRT2, and SIRT3, with IC50 values of 15, 10, and 33 μM, respectively

SIRT-IN-2 is a potent SIRT1/2/3 inhibitor [IC50s of 4, 1, and 7 μM, respectively].

SIRT-IN-3, a potent inhibitor of SIRT1 with an IC50 value of 17 μM, exhibits approximate 4-fold and 14-fold greater selectivity for SIRT1 over SIRT2 and SIRT3, with respective IC50 values of 74 μM for SIRT2 and 235 μM for SIRT3 [1].

Decapeptide-12, a competitive inhibitor of mushroom tyrosinase with an IC50 of 40 µM and a Kd of 61.1 μM for the C-terminal residue of tyrosinase, is a small oligopeptide that reduces melanin content in melanocytes by interacting with tyrosinase and increasing transcription of SIRT. It is utilized in researching melanogenesis, senescence, and inflammation [1] [2] [3].