1. Metabolic Enzyme/Protease
  2. Proteasome
  3. Rpn11-IN-1

Rpn11-IN-1 

Cat. No.: HY-101286
Handling Instructions

Rpn11-IN-1 is a potent and selective inhibitor of proteasome subunit Rpn11 with an IC50 of 390 nM.

For research use only. We do not sell to patients.

Rpn11-IN-1 Chemical Structure

Rpn11-IN-1 Chemical Structure

CAS No. : 2084867-65-0

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Description

Rpn11-IN-1 is a potent and selective inhibitor of proteasome subunit Rpn11 with an IC50 of 390 nM.

IC50 & Target

IC50: 390 nM (Rpn11)[1]

In Vivo

Rpn11 is a Zn2+-dependent metalloisopeptidase that hydrolyzes ubiquitin from tagged proteins that are trafficked to the proteasome for degradation. When inhibition of Rpn11-IN-1 (Compound 35) against Rpn11 is measured in the presence of Zn(cyclen)2+ (100 μM), a significant loss in activity against Rpn11 is observed (IC50=77.4 μM vs. 0.39 μM). The observed IC50 value shift is attributed to the ability of Zn(cyclen)2+ to compete/titrate Rpn11-IN-1 away from Rpn11. Rpn11-IN-1 blocks proliferation of tumor cells in culture. Rpn11-IN-1 has an IC50 of 2.1 μM and 3.8 μM against 293T and A549 cells, respectively[1].

Molecular Weight

315.41

Formula

C₁₅H₁₃N₃OS₂

CAS No.

2084867-65-0

SMILES

SC1=CC=CC2=C1N=CC(C(NCCC3=NC=CS3)=O)=C2

Shipping

Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Cell Assay
[1]

293T, A549 and HCT 116 cell lines are cultured in DMEM with 10% FBS in white, clear-bottom tissue culture-treated 96-well plates. Cells are treated with different concentrations of inhibitor compounds (e.g., Rpn11-IN-1; 0.01, 0.1, 1, 10, and 100 μM) in triplicates for 72 h at 37°C with 5% CO2 in air. CellTiter-Glo reagent is added to the 96 well plates to measure cell viability. Luminescence values are measured in PHERAstar microplate reader. Collected data is normalized to DMSO control and fit to a dose-response equation to determine IC50 values[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Rpn11-IN-1
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HY-101286
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