sirt2-in-1

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

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

SIRT2-IN-11 (AEM1) is a selective inhibitor of SIRT2 with an inhibitory concentration (IC50) of 18.5 μM. It induces apoptosis in a p53-dependent manner, activates the expression of CDKN1A, PUMA, and NOXA, and enhances the acetylation of p53. This compound is utilized in the study of p53-associated cancers.

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.

AK-1 is a sirtuin 2 (SIRT2) inhibitor (IC50:12.5 µM).that prevents hippocampal neurodegeneration in Alzheimer's disease models and induces cell cycle arrest in colon carcinoma cells.

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

OSS_128167 (SIRT6-IN-1) is a specific SIRT6 inhibitor, and for SIRT6(IC50=89 μM), SIRT1(IC50=1578 μM) and SIRT2(IC50=751 μM).

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].

Sirt1/2-IN-1 (Compound 7) is an inhibitor of SIRT1 and SIRT2, with IC50 values of 1.81 μg/mL for SIRT1, 2.10 μg/mL for SIRT2, and 20.5 μg/mL for SIRT3, and exhibits α-microtubulin hyperacetylation activity, demonstrating significant anticancer effects.

Sirt2-IN-5, a potent inhibitor of SIRT2, is specifically (2S)-2-[(Z)-4-(3-chlorophenyl)-3-methylbutanoylamino]-5-methylhexanoic acid [exact (1:1) of (2S,4R)-4-[(Z)-4-(3-chlorophenyl)-3-methylbutanoylamino]-5-methylhexanoic acid].

Nicotinamide-d4 is intended for use as an internal standard for the quantification of nicotinamide by GC- or LC-MS. Nicotinamide is an amide form of niacin, which is also known as vitamin B3, that can be biosynthesized in vivo or obtained through the diet. It is a precursor in the synthesis of the metabolic cofactor NAD+ and an inhibitor of sirtuin 1 (SIRT1; IC50 = <50 µM). Nicotinamide (10 µM) increases the activity of serine palmitoyltransferase (SPT) and the biosynthesis of ceramide, glucosylceramide, sphingomyelin, free fatty acids, and cholesterol in primary human keratinocytes. Nicotinamide (40 µM) induces apoptosis in SNU-398, SNU-739, and HepG2 hepatocellular carcinoma (HCC) cells, and it prevents the formation of neoplastic lesions in a diethylnitrosamine-induced mouse model of HCC. Unlike niacin, nicotinamide does not reduce plasma lipid levels or induce flushing.

Nicotinamide Hydrochloride, a form of vitamin B3 (niacin), inhibits sirtuin 2 (SIRT2) activity in vitro with an EC50 of 2 μM, reducing melanoma cell number by up to 90% and increasing cellular NAD+, ATP, and ROS levels. It also inhibits tumor growth in vivo and improves survival in melanoma-bearing mice, making it useful for skin cancer research, including melanoma.

SIRT1 2 3-IN-1 (compound 10) is a potent, selective, and cell-permeable inhibitor targeting SIRT1, SIRT2, and SIRT3, with inhibitory concentrations (IC50s) of 0.54 μM, 0.253 μM, and 0.72 μM, respectively. It is utilized in cancer research [1].

Sirt2-IN-7 (compound 22), a selective SIRT2 inhibitor with an IC50 of 178.2 nM and a Ki of 154.3 nM, is employed in cancer research [1].

Sirt1/2-IN-2 (compound hsa55) is a dual inhibitor, targeting SIRT1 with an IC50 of 1.8 μM and SIRT2 with an IC50 of 2.4 μM. It effectively inhibits p53 deacetylation while enhancing the acetylation of p53 and α-tubulin, promoting apoptosis and exhibiting anti-proliferative effects on human leukemia cell lines [1].

Sirt1/2-IN-3 (compound PS9) serves as a dual inhibitor of SIRT1/2, exhibiting IC50 values of 1.4 μM (SIRT1) and 2.0 μM (SIRT2), respectively. This compound effectively inhibits p53 deacetylation while simultaneously elevating p53 and α-tubulin acetylation levels. Additionally, Sirt1/2-IN-3 promotes apoptosis and exhibits antiproliferative effects on human leukemia cell lines [1].

Sirt1 2-IN-4 (compound PS3) is a potent triple inhibitor of SIRT1, SIRT2, and SIRT3, exhibiting IC50 values of 1.2 μM (SIRT1), 1.9 μM (SIRT2), and 18.6 μM (SIRT3), respectively. It effectively inhibits p53 deacetylation, indicating potential anticancer properties [1].

Mz325 serves as a dual inhibitor of both HDAC and Sirt2, exhibiting an IC50 of 9.7 µM against Sirt2, which are implicated in the pathogenesis of cancer and neurodegenerative diseases [1].