DZNep

SKU: orb1300836

Description

3-Deazaneplanocin A HCl is a dual-action small molecule inhibitor targeting both S-adenosyl-L-homocysteine hydrolase (SAHH) and the histone methyltransferase EZH2. It is utilized in epigenetic research to modulate histone methylation and cellular differentiation processes in both in vitro and in vivo experimental models.

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 120964-45-6
• MW: 298.7
• Purity: >98%
• Formula: C₁₂H₁₄N₄O₃ • HCl
• SMILES: Cl.Nc1nccc2n(cnc12)C1C=C(CO)C(O)C1O
• Target: Protein methyltransferase
• Solubility: Soluble in DMSO (up to 40 mg/ml).

Bioactivity

• 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.
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• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

3-Deazaneplanocin A; NSC 617989

Compound Identifiers

PubChem CID

358176