SirReal2

SirReal2 is a potent, isotype-selective Sirt2 inhibitor with an IC50 value of 140 nM and has very little effect on the activities of Sirt3-5. SirReal2 leads to tubulin hyperacetylation in HeLa cells and induces destabilization of the checkpoint protein BubR1. SirReal2 combined with VS-5584 (HY-16585) suppresses tumor growth and extends the survival rate of mice in tumor xenograft model. SirReal2 is is promising for research of cancer, inflammation and neurodegeneration[1][2][3][4].

Product Specifications

CAS Number

[709002-46-0]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Sirtuin

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics

Applications

Neuroscience-Neuromodulation

Field of Research

Cancer; Inflammation/Immunology; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/sirreal2.html

Purity

99.0

Solubility

DMSO : 31.25 mg/mL (ultrasonic)

Smiles

O=C(NC1=NC=C(CC2=C3C=CC=CC3=CC=C2)S1)CSC4=NC(C)=CC(C)=N4

Molecular Formula

C22H20N4OS2

Molecular Weight

420.55

Precautions

H302, H315, H319, H335

References & Citations

[1]Rumpf T, et al. Selective Sirt2 inhibition by ligand-induced rearrangement of the active site. Nat Commun. 2015 Feb 12;6:6263.|[2]Schiedel M, et al. Structure-Based Development of an Affinity Probe for Sirtuin 2. Angew Chem Int Ed Engl. 2016;55 (6) :2252-2256. |[3]Luo Y, et al. SIRT2 inhibitor SirReal2 enhances anti-tumor effects of PI3K/mTOR inhibitor VS-5584 on acute myeloid leukemia cells. Cancer Med. 2023 Sep;12 (18) :18901-18917.|[4]Zhang M, et al. SIRT2 promotes murine melanoma progression through natural killer cell inhibition. Sci Rep. 2021 Jun 21;11 (1) :12988.