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Proteasome inhibitor IX

CAS No. : 856849-35-9

MCE 站：Proteasome inhibitor IX

产品活性：Proteasome inhibitor IX (PS-IX; AM114) 是一种 Chalcone 衍生物，也是一种 20S 蛋白酶体 (20S proteasome) 的胰凝乳蛋白酶样活性抑制剂，IC₅₀ 值约为 1 μM。Proteasome inhibitor IX 具有 HCT116 p53^+/+ 细胞生长抑制活性，IC₅₀ 值为 1.49 μM，具有有效的抗癌活性。

研究领域：Metabolic Enzyme/Protease

作用靶点：Proteasome

In Vitro: Proteasome inhibitor IX (AM114; 0.1-10 ?M; 14 days; HCT116 p53^+/+ cells) treatment causes a loss of cell survival in the p53^+/+ and p53^-/- cells by approximately 70 and 20%, respectively at a concentration of 1 ?M.
Proteasome inhibitor IX (AM114) exhibits potent activity against p53^+/+ cells in colony formation assay, with an IC₅₀ value of 0.6 ?M.
Incubation of HCT116 p53^+/+ cells with 1 ?M Proteasome inhibitor IX (AM114) causes 28% of the cells to exhibit positive Annexin V staining at 48 h, and this fraction of dead cells increased to 76% at 72 h.
Proteasome inhibitor IX (AM114) treatment inhibits the chymotrypsin-like activity of the 20S proteasome in vitro, leading to a significant accumulation of ubiquitinated p53 and other cellular proteins in whole cells.

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