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CAS No. : 120964-45-6
MCE 国际站:3-Deazaneplanocin A hydrochloride
产品活性:3-Deazaneplanocin A hydrochloride (DZNep hydrochloride) 是一种有效的组蛋白甲基转移酶 (EZH2) 抑制剂。3-Deazaneplanocin A hydrochloride 是一种有效的 S-腺苷同型半胱氨酸水解酶 (AHCY) 抑制剂。3-Deazaneplanocin A hydrochloride 还具有抗正痘病毒 (orthopoxvirus) 和抗天花病毒活性。
研究领域:Epigenetics | Anti-infection
作用靶点:Histone Methyltransferase | Orthopoxvirus
In Vitro: 3-Deazaneplanocin A (DZNep) hydrochloride 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/G1 phase (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.
3-Deazaneplanocin A (DZNep) hydrochloride 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).
3-Deazaneplanocin A (DZNep) hydrochloride 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 IC0 values of 1.0±0.3 and 0.10±0.03 μM, respectively. 3-Deazaneplanocin A (DZNep) hydrochloride causes dose-dependent inhibition of cell proliferation of NSCLC cell lines, and the IC0 values range from 0.08 to 0.24 μM.
In Vivo: 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 (DZNep) and LBH589 (PS) compare to treatment with PS, 3-Deazaneplanocin A. 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 (DZNep) 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.
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