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UK-101 is a potent and selective inhibitor of the immunoproteasome LMP2, inhibiting β1i (LMP2), β1c (LMP2), and β5 (LMP2), with IC50s of 104 nM, 15 μM, and 1 μM, respectively. UK-101 exhibits a 144-fold and 10-fold higher affinity for β1i than for the distribution of β1c and β5 subunits. UK-101 induces apoptosis and can be used to study prostate cancer-related diseases.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $410 | In Stock | |
5 mg | $963 | In Stock | |
10 mg | $1,290 | In Stock | |
25 mg | $1,860 | In Stock | |
50 mg | $2,380 | In Stock |
Description | UK-101 is a potent and selective inhibitor of the immunoproteasome LMP2, inhibiting β1i (LMP2), β1c (LMP2), and β5 (LMP2), with IC50s of 104 nM, 15 μM, and 1 μM, respectively. UK-101 exhibits a 144-fold and 10-fold higher affinity for β1i than for the distribution of β1c and β5 subunits. UK-101 induces apoptosis and can be used to study prostate cancer-related diseases. |
Targets&IC50 | Immunoproteasome β5:1 μM , LMP2:104 nM , Immunoproteasome β1c:15 μM , LMP2:104 nM, Immunoproteasome β1c:15 μM, Immunoproteasome β5:1 μM |
In vitro | In the G1 phase of the cell cycle, UK-101 (2-8 μM; 24 hours) induces cell cycle arrest and increases the number of the PC-3 cell arrest.UK-101 (1-8 μM; 24 hours) induces cell accumulation in the G1 phase of the cell cycle, it increases p27 accumulation and significantly increases PARP cleavage as a dose-dependent manner.[1] |
In vivo | Tumor volume as a dose-dependent manner decreased by UK-101 (1-3 mg/kg; twice a week; 3 weeks)intraperitoneal injection, it significantly decreases tumor volume at a dose of 3 mg/kg. Additionally, UK-101-treated mice are suffering less systemic toxicity and the weights of mice treated with UK-101 remain steady over the 3-week treatment period.[1] |
Alias | UK101, UK 101 |
Molecular Weight | 484.74 |
Formula | C25H48N2O5Si |
Cas No. | 1000313-40-5 |
Smiles | C([C@@H](NC([C@@H](NC(CCCCCC)=O)C)=O)CC(C)C)(=O)[C@@]1(CO[Si](C(C)(C)C)(C)C)CO1 |
Relative Density. | 1.009 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (103.15 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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