PR-619

Catalog No.S7130

For research use only.

PR-619 is a non-selective, reversible inhibitor of the deubiquitinylating enzymes (DUBs) with EC50 of 1-20 μM in a cell-free assay. PR-619 activates autophagy.

PR-619 Chemical Structure

CAS No. 2645-32-1

Selleck's PR-619 has been cited by 41 publications

Purity & Quality Control

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Biological Activity

Description PR-619 is a non-selective, reversible inhibitor of the deubiquitinylating enzymes (DUBs) with EC50 of 1-20 μM in a cell-free assay. PR-619 activates autophagy.
Targets
JOSD2 [1]
(Cell-free assay)
SENP6 core [1]
(Cell-free assay)
UCH-L3 [1]
(Cell-free assay)
USP4 [1]
(Cell-free assay)
USP8 [1]
(Cell-free assay)
Click to View More Targets
1.17 μM(EC50) 2.37 μM(EC50) 2.95 μM(EC50) 3.93 μM(EC50) 4.90 μM(EC50)
In vitro

PR-619 is a cell-permeable pyridinamine class broad-spectrum DUB inhibitor whose known targets include ATXN3, BAP1, JOSD2, OTUD5, UCH-L1, UCH-L3, UCH-L5/UCH37, USP1, 2, 4, 5, 7, 8, 9X, 10, 14, 15, 16, 19, 20, 22, 24, 28, 47, 48, VCIP135, YOD1, as well as deISGylase PLpro, deNEDDylase DEN1, and deSUMOlyase SENP6. PR-619 are shown to increase overall protein polyubiquitination in HEK293T cells in a dose- and time-dependent manner (20 to 150 μM, 0.5 to 20 h). PR619 treatment results in upregulation of both K 48 - and K63-linked polyUb chains. PR-619 induces HCT116 cell death with EC50 values of 6.3 μM.[1]

Assay
Methods Test Index PMID
Western blot FOXM1 30865895

Protocol (from reference)

Kinase Assay:[1]
  • Ub-PLA2 assay:

    Recombinant enzymes in 20 mM Tris-HCl, pH 8.0, 2 mM CaCl2 and 2 mM β-mercaptoethanol (DUB assay buffer) are preincubated with single doses or dose ranges of PR-619 or P22077 for 30 minutes in a 96 well plate before the addition of Ub-PLA2 and NBD C6-HPC. The liberation of a fluorescent product within the linear range of the assay is monitored at room temperature using a fluorescence plate reader. Vehicle (2%(v/v) DMSO) and 10 mM N-ethylmaleimide are included as controls. Where ≥60% inhibition is observed, EC50 values are determined using a sigmoidal dose response equation.

Cell Research:[1]
  • Cell lines: HCT116, HEK293T
  • Concentrations: 0.5-50 μM
  • Incubation Time: 72 h
  • Method: 72 h hours later, 0.2 mg/mL resazurin prepared in phosphate-buffered saline is added to each well and the cells are incubated for an additional 3-6 h. The fluorescence of the resazurin reduction product is measured using Ex=535 nm and Em=590 nm filters on a fluorimeter. The EC50 values are calculated in Prism.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 223.28
Formula

C7H5N5S2

CAS No. 2645-32-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=C(C(=NC(=C1SC#N)N)N)SC#N

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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