AK-7 is a selective cell- and brain-permeable SIRT2 inhibitor, with an IC50 of 15.5 μM.
IC50&Target
SIRT2
15.5 μM (IC50)
体外研究
AK-7 (10 μM) reduces cholesterol levels in naive N2a neuroblastoma cells and hippocampal slice cultures from wild-type mice. AK-7 (1 μM) shows neuroprotective effect of AK-7 in striatal Huntington’s disease (HD) neurons. AK-7 (12.5 μM) decreases ratio of DA neurons in primary midbrain cultures.
体内研究
AK-7 (15 mg/kg/dose, i.p.) is brain-permeable in wild-type and HD mice. AK-7 (10, 20 mg/kg, i.p.) improves the behavior and neuropathological phenotype and extends survival of R6/2 HD mice. AK-7 (20 mg/kg) ameliorates HD neuropathology in R6/2 mice. AK-7 also reduces the polyglutamine aggregation in R6/2 brain. In addition, AK-7 treated 140CAG mice show motor performance changes that parallel untreated wild-type mice, with the 20 mg/kg dose being most effective and significantly different from untreated 140CAG mice.
分子式
C19H21BrN2O3S
分子量
437.35
CAS号
420831-40-9
运输条件
Room temperature in continental US; may vary elsewhere.