Powder: -20°C for 3 years | In solvent: -80°C for 1 year
3-deazaneplanocin A HCl is both an S-adenosyl-l-homocysteine hydrolase inhibitor and an enhancer of zeste homolog 2(EZH2) inhibitor.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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1 mg | 在庫あり | ¥ 20,000 | |||
5 mg | 在庫あり | ¥ 75,000 | |||
10 mg | 在庫あり | ¥ 104,500 | |||
25 mg | 在庫あり | ¥ 186,500 | |||
50 mg | 在庫あり | ¥ 273,500 | |||
100 mg | 在庫あり | ¥ 374,000 |
説明 | 3-deazaneplanocin A HCl is both an S-adenosyl-l-homocysteine hydrolase inhibitor and an enhancer of zeste homolog 2(EZH2) inhibitor. |
In vitro | 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]. |
In vivo | 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]. |
分子量 | 298.73 |
分子式 | C12H15ClN4O3 |
CAS No. | 120964-45-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 50 mg/mL (167.38 mM), Sonification is recommended.
You can also refer to dose conversion for different animals. 詳細
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3-deazaneplanocin A HCl 120964-45-6 Chromatin/Epigenetic Others Histone Methyltransferase 3-Deazaneplanocin A DZNep NSC-617989 3-Deazaneplanocin NSC617989 NSC 617989 3 deazaneplanocin A HCl Inhibitor Orthopoxvirus inhibit 3deazaneplanocin A HCl inhibitor