PROTAC Sirt2 Degrader-1

PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide Cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1/Sirt3 (IC50s>100 μM) [1].

Product Specifications

CAS Number

[2098487-75-1]

UNSPSC

12352005

Target

PROTACs; Sirtuin

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/PROTAC_Sirt2_Degrader-1.html

Purity

98.71

Solubility

DMSO : ≥ 100 mg/mL

Smiles

O=C(N(C(CCC1=O)C(N1)=O)C2=O)C(C2=CC=C3)=C3OCC(NCCCCN4C=C(COC5=CC(CC6=CN=C(NC(CSC7=NC(C)=CC(C)=N7)=O)S6)=CC=C5)N=N4)=O

Molecular Formula

C40H40N10O8S2

Molecular Weight

852.94

References & Citations

[1]Schiedel M, et al. Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals) . J Med Chem. 2018 Jan 25;61 (2) :482-491.