| Name | 3-deazaneplanocin A HCl |
| Description | 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 induced by HL-60 cells significantly increased when treated with 3-deazaneplanocin A HCl and PS compared to PS, 3-deazaneplanocin A HCl, or vehicle alone (P < .05). Cotreatment did not increase weight loss. Median survival: control, 36 days; PS, 42 days; 3-deazaneplanocin A HCl, 43 days; 3-deazaneplanocin A HCl plus PS, 52 days. Combined treatment improved survival of NOD/SCID mice with leukemia caused by AML HL-60 cells[3]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | H2O : 50 mg/mL (167.38 mM), Sonication is recommended.
DMSO : 50 mg/mL (167.38 mM)
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| Keywords | Histone Methyltransferase | 3-deazaneplanocin A HCl | 3-Deazaneplanocin A | DZNep | NSC-617989 | 3-Deazaneplanocin | NSC617989 | NSC 617989 | 3 deazaneplanocin A HCl | Inhibitor | Orthopoxvirus | inhibit | 3deazaneplanocin A HCl |
| Inhibitors Related | BIX-01294 trihydrochloride | Tazemetostat | Piribedil | XY1 | UNC 0631 | GSK126 | EPZ015666 | AMI-1 free acid | MS37452 | MRTX-1719 |
| Related Compound Libraries | Histone Modification Compound Library | Bioactive Compound Library | Epigenetics Compound Library | Inhibitor Library | Bioactive Compounds Library Max |
United States
