|4-溴-N'-丁基苯甲酰肼|CsnPharm

CAS No.: 537672-41-6

UF010/4-溴-N'-丁基苯甲酰肼 Catalog No. CSN17250

Synonyms: UF010

UF010 is a selective inhibitor of HDAC3, 2, 1 and 8 with IC50s of 0.06 μM, 0.1 μM, 0.5 μM and 1.5 μM, respectively.

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400-920-2911

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技术信息

生物活性

描述Histone deacetylases (HDACs) remove the acetyl group from lysine residues of histones and other cellular proteins. Heightened HDAC activities are implicated in several disorders including chronic neurologic, inflammatory and metabolic conditions. UF010 is class I HDAC-selective with IC₅₀s of 0.46, 1.33 and 0.19 μM against HDACs 1–3, respectively. In HCT116 cells, UF010 (2 μM for 1 h) consistently induced the accumulation of acetylated histones at all sites examined. Further, UF010 (2 μM) induced accumulation of acetylated p53 in both HCT116 and A549 cells after exposure to etoposide that inhibits DNA topoisomerase II, and induces double-stranded DNA breaks. It also notably stabilized p53 with or without etoposide treatment. It inhibited proliferation of the NCI-60 panel of cancer cell lines (including five breast cancer and seven colon cancer cell lines) with a mean GI₅₀ of 2.94 μM. In MDA-MB-231 cells, UF010 mainly blocked G1/S transition with an increased G1 cell population and a reduced cell population in the S phase in a dose-dependent manner. Moreover, UF010 at 1 μM markedly slowed cell migration which is associated with metastatic progression^[2].
作用机制The butyl side chain of UF010 fills a deep hydrophobic (“foot”) pocket^[2].
参考文献

[1] Wang Y, Stowe RL, et al. Identification of histone deacetylase inhibitors with benzoylhydrazide scaffold that selectively inhibit class I histone deacetylases. Chem Biol. 2015 Feb 19;22(2):273-284.
[2] Wang Y, Stowe RL, Pinello CE, et al. Identification of histone deacetylase inhibitors with benzoylhydrazide scaffold that selectively inhibit class I histone deacetylases. Chem Biol. 2015;22(2):273-284

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
- 3.6879 mL
- 18.4397 mL
- 36.8795 mL
- 5 mM
- 0.7376 mL
- 3.6879 mL
- 7.3759 mL
- 10 mM
- 0.3688 mL
- 1.8440 mL
- 3.6879 mL

技术信息

CAS号

537672-41-6

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C11H15BrN2O

运输

蓝冰

分子量

271.15

别名

UF010

溶解度

DMSO	400.0 mg/mL (1475.2 mM)
Water	insoluble

动物实验配方

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UF010/4-溴-N'-丁基苯甲酰肼 Catalog No. CSN17250

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