PROTAC Sirt2 Degrader-1

Modify Date: 2024-01-17 14:51:27

PROTAC Sirt2 Degrader-1 Structure
PROTAC Sirt2 Degrader-1 structure
Common Name PROTAC Sirt2 Degrader-1
CAS Number 2098487-75-1 Molecular Weight 852.94
Density N/A Boiling Point N/A
Molecular Formula C40H40N10O8S2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of 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 thalidomide, 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].

 Names

Name PROTAC Sirt2 Degrader-1

 PROTAC Sirt2 Degrader-1 Biological Activity

Description 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 thalidomide, 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].
Related Catalog
Target

SIRT2:0.25 μM (IC50)

In Vitro PROTAC Sirt2 Degrader-1 (Compound 12; 10 µM, 1-6 hours) induces Sirt2 degradation in HeLa cells[1]. Western Blot Analysis[1] Cell Line: HeLa cells Concentration: 10 µM Incubation Time: 1-6 hours Result: Caused Sirt2 degradation, but showed no effect on Sirt1 levels.
References

[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.

 Chemical & Physical Properties

Molecular Formula C40H40N10O8S2
Molecular Weight 852.94
Storage condition 2-8℃