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UK-101

(Synonyms: UK101, UK 101) Copy Product Info
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Synonyms: UK101, UK 101

Catalog No. T13247 Copy Product Info
Purity: 99.08%
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UK-101 is a small molecule inhibitor and a selective inhibitor of the immunoproteasome β1i (LMP2) subunit (IC50=104 nM), with 144-fold and 10-fold selectivity over the β1c and β5 subunits, respectively. This compound can induce apoptosis, possesses antitumor activity, and can be used for prostate cancer-related research.
UK-101
Cas No. 1000313-40-5
Pack SizePriceUSA StockGlobal StockQuantity
1 mg$239In StockIn Stock
5 mg$446In StockIn Stock
10 mg$718In StockIn Stock
25 mg$1,450In StockIn Stock
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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Purity:99.08%
ee:99.42%
Color:White
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Product Introduction

Bioactivity
Description
UK-101 is a small molecule inhibitor and a selective inhibitor of the immunoproteasome β1i (LMP2) subunit (IC50=104 nM), with 144-fold and 10-fold selectivity over the β1c and β5 subunits, respectively. This compound can induce apoptosis, possesses antitumor activity, and can be used for prostate cancer-related research.
Targets & IC50
Immunoproteasome β1c:15 μM, LMP2:104 nM, Immunoproteasome β5:1 μM
In vitro
Methods: PC-3 cells were treated with various concentrations of UK-101 (1-8 μM) for 24 hours, and cell cycle distribution, p27 protein accumulation, and PARP cleavage were detected.
Results: UK-101 induced cell cycle arrest at the G1 phase, increased the number of cells in the G1 phase, enhanced p27 protein accumulation, and significantly increased PARP cleavage in a dose-dependent manner.[1]
In vivo
Methods: To detect the in vivo antitumor activity and toxicity of UK-101, tumor-bearing mice were intraperitoneally injected with UK-101 (1-3 mg/kg, twice weekly for 3 weeks), tumor volume changes were measured, and mouse body weight was monitored.
Results: UK-101 treatment reduced tumor volume in a dose-dependent manner, with significant tumor volume reduction at the 3 mg/kg dose; meanwhile, mouse body weight remained stable during the treatment period, indicating low systemic toxicity.[1]
SynonymsUK101, UK 101
Chemical Properties
Molecular Weight484.74
FormulaC25H48N2O5Si
Cas No.1000313-40-5
SmilesC([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 & Solubility Information
StoragePure 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 recommended.
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
1mg5mg10mg50mg
1 mM2.0630 mL10.3148 mL20.6296 mL103.1481 mL
5 mM0.4126 mL2.0630 mL4.1259 mL20.6296 mL
10 mM0.2063 mL1.0315 mL2.0630 mL10.3148 mL
20 mM0.1031 mL0.5157 mL1.0315 mL5.1574 mL
50 mM0.0413 mL0.2063 mL0.4126 mL2.0630 mL
100 mM0.0206 mL0.1031 mL0.2063 mL1.0315 mL
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Keywords

Related Tags: UK-101 chemical structure | UK-101 in vivo | UK-101 in vitro | UK-101 formula | UK-101 molecular weight