Ivaltinostat

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Ivaltinostat formic

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MCE 国际站：Ivaltinostat formic

产品活性：Ivaltinostat (CG-200745) formic 是一种口服有效的泛 HDAC 抑制剂，具有异羟肟酸部分，可在催化袋底部结合锌。Ivaltinostat formic 抑制组蛋白 H3 和微管蛋白的脱乙酰作用。Ivaltinostat formic 诱导 p53 的积累，促进 p53 依赖性反式激活，并增强 MDM2 和 p21 (Waf1/Cip1) 蛋白的表达。Ivaltinostat formic 可增强 Gemcitabine 耐药细胞对 Gemcitabine (HY-16138) 和 5-Fluorouracil (5-FU; HY-90006) 的敏感性。Ivaltinostat formic 诱导凋亡并具有抗肿瘤作用。

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

作用靶点：HDAC  |  MDM-2/p53  |  Apoptosis

In Vitro: Ivaltinostat (CG-200745; 0.01-100 μM; 48 hours) formic inhibits growth of prostate cancer cells (LNCaP, DU145 and PC3 cells). Ivaltinostat (1, 10 μM; 24, 48 hours) formic increases sub-G1 population, and activates caspase-9, -3 and -8.
Ivaltinostat (0.001-100 μM; for 72 hours) inhibits proliferation of cholangiocarcinoma cells (IC₅₀s of 0.63, 0.93, and 1.80 μM for SNU-1196, SNU-1196/GR, SNU-308 cells, respectively).
Ivaltinostat (0-10 μM; 48 hours) formic reduces the Calu6 cells proliferation to 40% of untreated cells.
Ivaltinostat (3 μM; 1-24 hours) formic significantly increases Calu6 cells proportion in G2/M phase (69%).
Ivaltinostat (0-10 μM; 1-24 hours) formic treatment with low concentration significantly increases the acetylation of histone H3 and H4 in Calu6 cells at various sites in a time-dependent manner up to 24 hours after treatment.

In Vivo: Ivaltinostat (CG-200745; p.o.; 30 mg/kg/day; for 7 days) formic attenuates oxidative stress, inflammatory cytokines, and adhesion molecules in UUO kidneys.

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