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UK-101

Chemical Structure : UK-101

CAS No.: 1000313-40-5

UK-101 (UK 101, UK101)

Catalog No.: PC-60966Not For Human Use, Lab Use Only.

UK-101 is a potent, specific immunoproteasome β1i (LMP2) subunit inhibitor with IC50 of 104 nM, 144- and 10-fold selectivity over β1c and β5 subunit respectivey.

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Biological Activity

UK-101 is a potent, specific immunoproteasome β1i (LMP2) subunit inhibitor with IC50 of 104 nM, 144- and 10-fold selectivity over β1c and β5 subunit respectivey.
UK-101 induces apoptosis of PC-3 cells and results in significant inhibition (~50-60%) of tumour growth in vivo.
UK-101 does not block degradation of IκBα in PC-3 cells treated with TNF-α.

Physicochemical Properties

M.Wt 484.753
Formula C25H48N2O5Si
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-((S)-1-(((S)-1-((S)-2-(((tert-butyldimethylsilyl)oxy)methyl)oxiran-2-yl)-4-methyl-1-oxopentan-2-yl)amino)-1-oxopropan-2-yl)heptanamide

References

1. de Bruin G, et al. J Med Chem. 2014 Jul 24;57(14):6197-209.

2. Wehenkel M, et al. Br J Cancer. 2012 Jun 26;107(1):53-62.

3. Lei B, et al. J Phys Chem B. 2010 Sep 30;114(38):12333-9.

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