Entinostat恩替诺特,209783-80-2

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Entinostat

CAS No. : 209783-80-2

MCE 国际站：Entinostat

产品活性：Entinostat 选择性，可口服的 HDAC class I 抑制剂，抑制 HDAC1，HDAC2 和 HDAC3 的 IC₅₀ 分别为 243 nM，453 nM 和 248 nM。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics  |  Autophagy  |  Apoptosis

作用靶点：HDAC  |  Autophagy  |  Apoptosis

In Vitro: Binding affinity of Entinostat (MS-275) against HDAC1 and HDAC2 is 282 nM and 156 nM, respectively. Effects of the HDAC inhibitor Entinostat (MS-275) have been examined in human leukemia and lymphoma cells (U937, HL-60, K562, and Jurkat) as well as in primary acute myelogenous leukemia blasts in relation to differentiation and apoptosis. MS-275 displays dose-dependent effects in each of the cell lines. When administered at a low concentration (e.g., 1 μM), MS-275 exhibits potent antiproliferative activity, inducing p21CIP1/WAF1-mediated growth arrest and expression of differentiation markers (CD11b) in U937 cells. Entinostat (MS-275) potently induces cell death, triggering apoptosis in ~70% of cells at 48 h.

In Vivo: Entinostat (MS-27-275) at 49 mg/kg shows marked antitumor effects against KB-3-1, 4-1St, and St-4 tumor lines, and a moderate effect against Capan-1 tumor. Entinostat at 24.5 mg/kg and 12.3 mg/kg also shows significant effects against these tumors. In addition, oral administration of Entinostat apparently increases the level of histone acetylation in HT-29 tumor xenografts 4-24 h after the administration. MS-275 administration (3.5 mg/kg i.p.) to Experimental autoimmune neuritis (EAN) rats once daily from the appearance of first neurological signs greatly reduces the severity and duration of EAN and attenuated local accumulation of macrophages, T cells and B cells, anddemyelination of sciatic nerves. In addition, MS-275 treatment increases proportion of infiltrated Foxp3⁺ cells and anti-inflammatory M2 macrophages in sciatic nerves of EAN rats.

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