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CAS No.: 1403783-31-2

Nexturastat A Catalog No. CSN15915

Synonyms: Nexturastat A

Nexturastat A is a selective inhibitor of HDAC6 with IC50 of 5 nM.

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实验方案

技术信息

生物活性

靶点 HDAC6

IC50:5nM
描述Histone deacetylases (HDACs) participate in the control of cellular biological processes via specificly removing acetyl groups on lysine residues in histones and non-histone proteins. The isoform of HDAC6 is orientated in the cytoplasm and mainly interacts with non-histone proteins. It plays a central role in microtubule-dependent cell motility via deacetylation of tubulin. In addition to its protein deacetylase activity, HDAC6 plays a key role in the degradation of misfolded proteins. Nexturastat A is a HDAC6 selective inhibitor with IC₅₀ of 5.02nM, while the IC₅₀s of it against HDAC1, 2, 3, 4, 5, 7, 8, 9, 10, 11 were 3.02μM, 6.92μM, 6.68μM, 9.39μM, 11.7μM, 4.46μM, 0.95μM, 6.72μM, 7.57μM and 5.14μM, respectively^[3]. Treatment of B16 cells with Nexturastat A at doses ranging from 1nM to 10000nM concentration dependently increased acetyl-tubulin levels^[3]. 10μM, 20μM , 30μM and 40μM Nexturastat A dose-dependently impaired the viability of multiple myeloma PRMI-8226 and U266 cell lines. 48h treatment of Nexturastat A at the concentration of 40μM induced apoptosis in RPMI-8226 and U266 cells^[4]. In SM1 murine melanoma tumor model established in C57BL/6 mice, Nexturastat A was administrated 5 times a week at the dose of 15mg/kg, or in combination of anti-PD-1 for 25 days. At day25, the tumor volume of the combination group, Nexturastat A group, anti-PD-1 group and control group were 257.3mm³, 750.1 mm³, 1030 mm³ and 2034 mm³, respectively^[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
- 2.9291 mL
- 14.6454 mL
- 29.2908 mL
- 5 mM
- 0.5858 mL
- 2.9291 mL
- 5.8582 mL
- 10 mM
- 0.2929 mL
- 1.4645 mL
- 2.9291 mL

技术信息

CAS号

1403783-31-2

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H23N3O3

运输

蓝冰

分子量

341.40

别名

Nexturastat A

溶解度

DMSO	67.0 mg/mL (196.2 mM)
Water	Insoluble
Ethanol	2.0 mg/mL (5.9 mM)

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