NKL 22

A selective HDAC1/3 inhibitor

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库存: 现货

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促销价

数量
5mg

￥400.00

320.00

- +
10mg

￥650.00

520.00

- +
25mg

￥1375.00

1100.00

- +
50mg

￥2612.00

2090.00

- +
100mg

￥4750.00

3800.00

- +

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Background

PAOA is a selective histone deacetylase (HDAC) inhibitor with IC₅₀ values of 199 and 69 nM for HDAC1 and HDAC3, respectively.¹ It is selective for HDAC1 and HDAC3, having IC₅₀ values greater than 1.59 μM for HDAC2, 4, 5, 7, and 8 in a cell-free enzyme assay. In vitro, PAOA induces histone H3 and H4 hyperacetylation.² PAOA improves the metabolic deficit exhibited by murine striatal cells isolated from Hdh^Q111 knock-in mice in a dose-dependent manner and reduces eye neurodegeneration in a D. melanogaster model of Huntington’s disease.¹ In vivo, PAOA prevents formation of Huntingtin (Htt) protein aggregates in the brain and reduces the cognitive deficits in the N171-82Q mouse model of Huntington’s disease.³

1.Jia, H., Pallos, J., Jacques, V., et al.Histone deacetylase (HDAC) inhibitors targeting HDAC3 and HDAC1 ameliorate polyglutamine-elicited phenotypes in model systems of Huntington's diseaseNeurobiol. Dis.46(2)351-361(2012) 2.Mai, A., Perrone, A., Nebbioso, A., et al.Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: Histone deacetylase inhibition and in-cell activitiesBioorg. Med. Chem. Lett.18(8)2530-2535(2008) 3.Jia, H., Kast, R.J., Steffan, J.S., et al.Selective histone deacetylase (HDAC) inhibition imparts beneficial effects in Huntington's disease mice: Implications for the ubiquitin-proteasomal and autophagy systemsHum. Mol. Genet.21(24)5280-5293(2012)