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3-deazaneplanocin A HCl

Catalog No. T6360 CAS 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.

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3-deazaneplanocin A HCl Chemical Structure

3-deazaneplanocin A HCl, CAS 120964-45-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 87.00
5 mg	In stock	$ 327.00
10 mg	In stock	$ 455.00
25 mg	In stock	$ 813.00
50 mg	In stock	$ 1,190.00
100 mg	In stock	$ 1,630.00

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Purity: 98.34%

Purity: 93.24%

Biological Description

Chemical Properties

Storage & Solubility Information

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 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].

Molecular Weight	298.73
Formula	C12H15ClN4O3
CAS No.	120964-45-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

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

References and Literature

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

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Histone Modification Compound Library Epigenetics Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Keywords

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

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