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3-deazaneplanocin A HCl

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Catalog No. T6360Cas No. 120964-45-6

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

3-deazaneplanocin A HCl

3-deazaneplanocin A HCl

🥰Excellent
Purity: 98.34%
Catalog No. T6360Cas No. 120964-45-6
3-deazaneplanocin A HCl is both an S-adenosyl-l-homocysteine hydrolase inhibitor and an enhancer of zeste homolog 2(EZH2) inhibitor.
Pack SizePriceAvailabilityQuantity
1 mg$87In Stock
5 mg$327In Stock
10 mg$455In Stock
25 mg$813In Stock
50 mg$1,190In Stock
100 mg$1,630In Stock
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Purity:98.34%
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Product Introduction

Bioactivity
Description
3-deazaneplanocin A (DZNeP)HCl, an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with Ki of 50 pM.
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].
Chemical Properties
Molecular Weight298.73
FormulaC12H15ClN4O3
Cas No.120964-45-6
SmilesCl.Nc1nccc2n(cnc12)C1C=C(CO)C(O)C1O
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -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)
Solution Preparation Table
H2O/DMSO
1mg5mg10mg50mg
1 mM3.3475 mL16.7375 mL33.4750 mL167.3752 mL
5 mM0.6695 mL3.3475 mL6.6950 mL33.4750 mL
10 mM0.3348 mL1.6738 mL3.3475 mL16.7375 mL
20 mM0.1674 mL0.8369 mL1.6738 mL8.3688 mL
50 mM0.0670 mL0.3348 mL0.6695 mL3.3475 mL
100 mM0.0335 mL0.1674 mL0.3348 mL1.6738 mL

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