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PROTAC Sirt2 Degrader-1

Names

[ CAS No. ]:
2098487-75-1

[ Name ]:
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]:

Signaling Pathways >> Epigenetics >> Sirtuin
Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> Sirtuin
Signaling Pathways >> PROTAC >> PROTAC

[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℃

Related Compounds