UK-101 

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: 104 nM (LMP2)
IC50: 15 μM (immunoproteasome β1c)
IC50: 1 μM (immunoproteasome β5)^[1]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

484.74

C₂₅H₄₈N₂O₅Si

1000313-40-5

Solid

White to off-white

O=C([C@]1(CO1)CO[Si](C)(C)C(C)(C)C)[C@H](CC(C)C)NC([C@H](C)NC(CCCCCC)=O)=O

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [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.  [Content Brief]

  [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.  [Content Brief]