UK-101,1000313-40-5

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UK-101

CAS No. : 1000313-40-5

MCE 国际站：UK-101

产品活性：UK-101 是一种强有力的和有选择性的免疫蛋白酶体 β1i (LMP2) 的抑制剂 (IC₅₀=104 nM)。UK-101 对 LMP2 的选择性是 β1c (IC₅₀=15 μM) 和 β5 (IC₅₀=1 μM) 亚基的 144 倍和 10 倍。UK-101 可以诱导细胞凋亡 (apoptosis)，可用于前列腺癌的相关研究。

研究领域：Metabolic Enzyme/Protease  |  Apoptosis

作用靶点：Proteasome  |  Apoptosis

In Vitro: UK-101 (2-8 μM; 24 hours) induces cell cycle arrest and increases the number of the PC-3 cells arrest in G1 phase of the cell cycle.
UK-101 (2-8 μM; 24 hours) induces cell apoptosis, shows a minimal increase in late apoptosis, but has no significant increase in early apoptosis.
UK-101 (1-8 μM; 24 hours) induces cells accumulation in the G1 phase of the cell cycle, it increases p27 accumulation and significantly increases PARP cleavage as a dose-dependent manner.

In Vivo: UK-101 (intraperitoneal injection; 1-3 mg/kg; twice a week; 3 weeks) decreases tumor volume as a dose-dependent manner, it significantly decreases tumor volume at a dose of 3 mg/kg. Additionally, UK-101-treated mice is suffering less systemic toxicity and the weights of mice treated with UK-101 remains steady over the 3-week treatment period.

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