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3-deazaneplanocin A HCl

3-deazaneplanocin A HCl 是组蛋白甲基转移酶 (EZH2) 和 S-腺苷同型半胱氨酸水解酶 (AHCY) 抑制剂。

CAS号

120964-45-6

分子式

C12H15ClN4O3

主要靶点

Others|Histone Methyltransferase

仅限科研使用

Cat No : CM04543

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Synonyms

验证数据展示

  • CAS No.: 120964-45-6

    3-deazaneplanocin A HCl
    CAS#: 120964-45-6

产品信息

3-deazaneplanocin A HCl is both an S-adenosyl-l-homocysteine hydrolase inhibitor and an enhancer of zeste homolog 2(EZH2) inhibitor.

CAS号 120964-45-6
分子式 C12H15ClN4O3
主要靶点 Others|Histone Methyltransferase
主要通路 表观遗传|其他
分子量 298.73
纯度 98.34%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

体内活性

The survival of NOD/SCID mice with AML due to HL-60 cells was significantly higher, if treated with 3-deazaneplanocin A HCl and PS compared to treatment with PS, 3-deazaneplanocin A HCl, or vehicle alone (P < .05). Cotreatment with 3-deazaneplanocin A HCl and PS also did not increase the weight loss in the mice. Median survival was as follows: control, 36 days; PS, 42 days; 3-deazaneplanocin A HCl, 43 days; and 3-deazaneplanocin A HCl plus PS, 52 days.Compared with treatment with each agent alone, combined treatment with 3-deazaneplanocin A HCl and PS improved survival of NOD/SCID mice with leukemia caused by the AML HL-60 cells[3].

体外活性

EZH2 expression was detected by quantitative PCR in 15 PDAC cells, including seven primary cell cultures, showing that expression values correlated with their originator tumors (Spearman R(2) = 0.89, P = 0.01). EZH2 expression in cancer cells was significantly higher than in normal ductal pancreatic cells and fibroblasts. The 3-deazaneplanocin A HCl(5 μmol/L, 72-hour exposure) modulated EZH2 and H3K27me3 protein expression and synergistically enhanced the antiproliferative activity of gemcitabine, with combination index values of 0.2 (PANC-1), 0.3 (MIA-PaCa-2), and 0.7 (LPC006). The drug combination reduced the percentages of cells in G(2)-M phase (e.g., from 27% to 19% in PANC-1, P < 0.05) and significantly increased apoptosis compared with gemcitabine alone. Moreover, 3-deazaneplanocin A HCl enhanced the mRNA and protein expression of the nucleoside transporters hENT1/hCNT1. 3-deazaneplanocin A HCl decreased cell migration, which was additionally reduced by 3-deazaneplanocin A HCl/gemcitabine combination (-20% in LPC006, after 8-hour exposure, P < 0.05) and associated with increased E-cadherin mRNA and protein expression. Furthermore, 3-deazaneplanocin A HCl and 3-deazaneplanocin A HCl/gemcitabine combination significantly reduced the volume of PDAC spheroids growing in CSC-selective medium and decreased the proportion of CD133+ cells[2].

溶解度

H2O:50 mg/mL (167.38 mM),Sonification is recommended.

参考文献

1.Glazer RI, et al. Biochem Pharmacol, 1986, 35(24), 4523-4527.
2.Fiskus W, et al. Blood, 2009, 114(13), 2733-2743.

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