420831-40-9|AK-7|CsnPharm

CAS No.: 420831-40-9

AK-7 Catalog No. CSN16491

Synonyms: CS-3223;GL-8955

AK-7 is a selective and brain-permeable SIRT2 inhibitor and is neuroprotective in Huntington disease mouse models.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Sirtuin 2 is a member of the sirtuin family of proteins. It is a NAD-dependent protein deacetylase, which deacetylates internal lysines on histone and alpha-tubulin as well as many other proteins such as key transcription factors. Sirtuin 2 participates in the modulation of multiple and diverse biological processes such as cell cycle control, genomic integrity, microtubule dynamics, cell differentiation, metabolic networks, and autophagy. It also plays a major role in the control of cell cycle progression and genomic stability. AK-7 is a Sirtuin 2 selective inhibitor with IC₅₀ of 15.5μM. At the concentration of 10μM, AK-7 reduced cholesterol levels in naive N2a neuroblastoma cells and hippocampal slice cultures from wild-type mice. At the concentration of 1μM , AK-7 showed neuroprotective effect in striatal Huntington's disease neurons^[3]. When i.p. administrated at the dose of 10mg/kg or 20mg/kg, AK-7 improved the behavior and neuropathological phenotype and extended survival of R6/2 HD mice. At the dose of 20mg/kg, AK-7 ameliorated HD neuropathology in R6/2 mice^[4]. At the dose of 20mg/kg, i.p. administrated AK7 was neuroprotective in a subacute MPTP mouse model of Parkinson's disease and significant increase of α-tubulin aectylation in the striatum after AK7 treatment was confirmed^[5].
作用机制AK-7 is a Sirtuin 2 selective inhibitor with a NAD⁺ competitive mechanism. The binding of AK-7 to Sirtuin 2 was suggested through docking calculations^[5].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2865 mL
- 11.4325 mL
- 22.8650 mL
- 5 mM
- 0.4573 mL
- 2.2865 mL
- 4.5730 mL
- 10 mM
- 0.2286 mL
- 1.1432 mL
- 2.2865 mL

技术信息

CAS号

420831-40-9

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H21BrN2O3S

运输

蓝冰

分子量

437.35

别名

CS-3223;GL-8955

溶解度

DMSO	90.0 mg/mL (205.8 mM)
Water	insoluble

动物实验配方

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靶点选择性

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