UF010

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Chemical Structure| 537672-41-6 同义名 : -
CAS号 : 537672-41-6
货号 : A796758
分子式 : C11H15BrN2O
纯度 : 99%+
分子量 : 271.154
MDL号 : MFCD03603083
存储条件：

Pure form Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(387.23 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.69mL

0.74mL

0.37mL

18.44mL

3.69mL

1.84mL

36.88mL

7.38mL

3.69mL
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