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3-Deazaneplanocin A

CAS No. : 102052-95-9

MCE 站：3-Deazaneplanocin A

产品活性：3-Deazaneplanocin A (DZNep) 是一种有效的组蛋白甲基转移酶 (histone methyltransferase，EZH2) 抑制剂。3-Deazaneplanocin A 是一种有效的 S-腺苷同型半胱氨酸水解酶 (AHCY) 抑制剂。

研究领域：Epigenetics

作用靶点：Histone Methyltransferase

In Vitro: 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/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 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 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±0.3 and 0.1±0.03 μM, respectively. 3-Deazaneplanocin A 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 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. 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.

相关产品：3-Deazaneplanocin A hydrochloride  |  Chaetocin  |  UNC0642  |  UNC1999  |  MS023  |  BIX-01294  |  EPZ020411 hydrochloride  |  MM-102 TFA  |  SGC0946  |  A-366  |  Amodiaquine dihydrochloride dihydrate  |  CM-272  |  AZ505  |  SGC707  |  PFI-2 hydrochloride  |  NSC 663284  |  UNC0379  |  A-196  |  Sinefungin  |  SGC3027  |  AMI-1  |  EI1  |  BVT948  |  MS049  |  HLCL-61 hydrochloride  |  UNC0646  |  UNC 0631  |  UNC3866

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