3-Deazaneplanocin A (DZNep) is a potenthistone methyltransferaseEZH2inhibitor^[1][2]. 3-Deazaneplanocin A is a potentS-adenosylhomocysteine hydrolase (AHCY)inhibitor. 3-Deazaneplanocin A shows anti-orthopoxvirus activity^[6][7].

EZH2^[1]

3-Deazaneplanocin A is a potent histone methyltransferase EZH2 inhibitor. Treatment of OCI-AML3 cells with 3-Deazaneplanocin A (1.0 μM) results in a significant increase in accumulation of cells in the G₀/G₁phase (58.5%) with a concomitant decrease in the number of cells in S phase (35.2%) and G₂/M phases (6.3%) of the cell cycle (P<0.05). Treatment with 3-Deazaneplanocin A (200 nM to 2.0 μM) for 48 hours, dose dependently, inhibits colony growth of OCI-AML3 and HL-60 cells^[1]. 3-Deazaneplanocin A reduces the expression of EZH2, especially after 72 hours (e.g. 48%, 32% and 36% reduction of EZH2 in PANC-1, MIA-PaCa-2 and LPc006 cells, respectively)^[2]. 3-Deazaneplanocin A shows minimal growth inhibition in PANC-1 cells. More than 50% of these cells are still growing after exposure at the highest concentration (20 μM). MIA-PaCa-2 and LPc006 cells are much more sensitive, with IC₀values of 1±0.3 and 0.1±0.03 μM, respectively^[2]. 3-Deazaneplanocin A causes dose-dependent inhibition of cell proliferation of NSCLC cell lines, and the IC₀values range from 0.08 to 0.24 μM^[3].

The survival of NOD/SCID mice with acute myeloid leukemia (AML) due to HL-60 cells is significantly higher, if treated with 3-Deazaneplanocin A and Panobinostat (PS) compare to treatment with PS, 3-Deazaneplanocin A, or vehicle alone (P<0.05). Median survival is as follows: control, 36 days; PS, 42 days; 3-Deazaneplanocin A, 43 days; and 3-Deazaneplanocin A plus PS, 52 days^[1]. There is a progressive increase in weight of rats treated with physiological saline in a time-dependent manner (the mean growth rate=3.19% per day). Administration of 20 mg/kg 3-Deazaneplanocin A not only markedly reduces the relative weight of the rats compare to the initial weight (–2.0%, –4.9% and –1.2%) in the first three days post-treatment, but also suppresses the weight growth rate to 2.6% per day from the fourth day onwards post-dose^[4].

262.26

Solid

C₁₂H₁₄N₄O₃

102052-95-9

3-去氮腺嘌呤A

Room temperature in continental US; may vary elsewhere.

• 1.

  3-Deazaneplanocin A (DZNep) is prepared in PBS^[5].