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DI-591

Catalog No. T11033 Copy Product Info
🥰Excellent
DI-591 is an effective, high-affinity and cell-permeability inhibitor for DCN1-UBC12 interaction. DI-591 binds to DCN1 and DCN2 with Ki values of 12 and nM and 10.4 nM, respectively, and has no obvious binding to DCN3, DCN4 and DCN5 proteins.

DI-591

Copy Product Info
🥰Excellent
Catalog No. T11033

DI-591 is an effective, high-affinity and cell-permeability inhibitor for DCN1-UBC12 interaction. DI-591 binds to DCN1 and DCN2 with Ki values of 12 and nM and 10.4 nM, respectively, and has no obvious binding to DCN3, DCN4 and DCN5 proteins.

DI-591
Cas No. 2245887-38-9
Pack SizePriceUSA StockGlobal StockQuantity
25 mg$1,4208-10 weeks8-10 weeks
50 mg$1,8508-10 weeks8-10 weeks
100 mg$2,9708-10 weeks8-10 weeks
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
DI-591 is an effective, high-affinity and cell-permeability inhibitor for DCN1-UBC12 interaction. DI-591 binds to DCN1 and DCN2 with Ki values of 12 and nM and 10.4 nM, respectively, and has no obvious binding to DCN3, DCN4 and DCN5 proteins.
In vitro
DI-591 binds to DCN1 and DCN2 with Ki values of 12 nM and 10.4 nM, respectively, and has no obvious binding to DCN3, DCN4 and DCN5 proteins. Therefore, DI-591 has a high binding affinity for recombinant human DCN1 and DCN2 proteins, and its selectivity is more than 1000 times that of recombinant human DCN3-5 protein [1]. DI-591 (0-10μM; 1 hour; KYSE70 cells) binds to the DCN1 and DCN2 proteins of the cells and disrupts the binding of the DCN1 and UBC12 proteins. DI-591 (10 μM; 24 hours; THLE2 cells) treatment can strongly increase the mRNA levels of NQO1 and HO1, resulting in the up-regulation of HO1 protein in the cells. It is worth noting that DI-591 has no effect on the mRNA level of NRF2. DI-591's selective inhibition of cullin 3's dienylation leads to the accumulation of NRF2 protein and its transcriptional activation. Knockdown experiments show that DCN1, but not DCN2, plays a key role in the regulation of dimerization of cullin 3 but not other cullins. DI-591 is an excellent probe compound for studying the role of cullin 3 CRL (Cullin-RING E3 ubiquitin ligase) in biological processes and human diseases.
Chemical Properties
Molecular Weight585.8
FormulaC31H47N5O4S
Cas No.2245887-38-9
SmilesCCC(=O)N[C@@H](Cc1nc2ccc(cc2s1)C(C)C)C(=O)N[C@H](CNC(=O)CCN1CCOCC1)C1CCCCC1
Relative Density.1.169 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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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:
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2 Enter the in vivo formulation:
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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