UK-101

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

UK-101 

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。

UK-101

UK-101 Chemical Structure

CAS No. : 1000313-40-5

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生物活性

UK-101 is a potent and selective immunoproteasome β1i (LMP2) inhibitor with an IC50 value of 104 nM, displays 144- and 10-fold selectivity over β1c (IC50=15 μM) and β5 subunit (IC50=1 μM), respectivey[1]. UK-101 induces cell apoptosis and can be used for the study of prostate cancer[2].

IC50 & Target

IC50: 104 nM (LMP2)
IC50: 15 μM (immunoproteasome β1c)
IC50: 1 μM (immunoproteasome β5)[1]
体外研究
(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[2].
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[2].
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[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: PC-3 cells
Concentration: 2 μM; 8 μM
Incubation Time: 24 hours
Result: Induced G1 cell cycle arrest in PC-3 cells.

Apoptosis Analysis[1]

Cell Line: PC-3 cells
Concentration: 2 μM; 8 μM
Incubation Time: 24 hours
Result: Increased cell apoptosis as a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: PC-3 cells
Concentration: 1 μM; 2 μM; 8 μM
Incubation Time: 24 hours
Result: Increased PARP cleavage and p27 accumulation as a dose-dependent manner.

体内研究
(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[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Subcutaneously implanted PC-3 cells in 6-week-old male BALB/c athymic nude mice[2]
Dosage: 1 mg/kg; 3 mg/kg
Administration: Intraperitoneal injection; twice a week; 3 weeks
Result: Inhibited tumour growth in the prostate cancer mouse xenograft model.

分子量

484.74

Formula

C25H48N2O5Si
CAS 号

1000313-40-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. de Bruin G, et al. Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes. J Med Chem. 2014 Jul 24;57(14):6197-209.

    [2]. Wehenkel M, et al. A selective inhibitor of the immunoproteasome subunit LMP2 induces apoptosis in PC-3 cells and suppresses tumour growth in nude mice. Br J Cancer. 2012 Jun 26;107(1):53-62.

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