SIRT2 Inhibitor, Inactive Control, AGK7

Description

AGK2 is a cell-permeable, selective inhibitor of SIRT2 (IC₅₀ = 3.5 μM) that minimally affects either SIRT1 or SIRT3 at 10-fold higher levels. AGK7 is an inactive control to be used in experiments with AGK2. It differs from AGK2, structurally, only in the position of nitrogen in the quinoline group. AGK7 has IC₅₀ values greater than 50 μM on SIRT1 and SIRT2 and greater than 5 μM on SIRT3.

Uses

AGK7 is a potent inhibitor of sirtuin 2 (SIRT2). AGK7 rescues alpha-synuclein toxicity and modified inclusion morphology in a cellular model of Parkinson's disease. AGK7 protects against dopaminergic cell death both in vitro and in a Drosophila model of Parkinson's disease[1].

References

[1]. outeiro tf, kontopoulos e, altmann sm, et al. sirtuin 2 inhibitors rescue alpha-synuclein-mediated toxicity in models of parkinson's disease. science. 2007 jul 27;317(5837):516-9.
[2]. cole pa. chemical probes for histone-modifying enzymes. nat chem biol. 2008 oct;4(10):590-7.