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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 | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $239 | In Stock | In Stock | |
| 5 mg | $446 | In Stock | In Stock | |
| 10 mg | $718 | In Stock | In Stock | |
| 25 mg | $1,450 | In Stock | 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 β1c:15 μM, Immunoproteasome β5:1 μM, LMP2:104 nM |
| 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] |
| Synonyms | 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 | Pure form: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 237.5 mg/mL (489.95 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+90% Corn Oil: 3.3 mg/mL (6.81 mM), Sonication is recommeded. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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