PR-619

PR-619

PR-619

Min.Order / FOB Price:Get Latest Price

100 Gram

FOB Price: USD 1.0000

  • Min.Order :100 Gram
  • Purity: 98%
  • Payment Terms : L/C

Keywords

PR-619 PR-619;2,6-DiaMino-3,5-dithiocyanopyridine;3,5-dithiocyanatopyridine-2,6-diaMine;Thiocyanic acid, C,C'-(2,6-diamino-3,5-pyridinediyl) ester;2,6-Diamino-3,5-dithiocyanopyridine PR 619;PR 619 2,6-Diamin 2645-32-1

Quick Details

  • Appearance:white solid
  • Application:CAS:2645-32-1; Small molecule inhibitors
  • PackAge:100g,500g,1kg,25kg/drum
  • ProductionCapacity:1000|Gram|Month
  • Storage:Dry seal
  • Transportation:shipping

Superiority:

We are specialized in custom synthesis, chemical/pharmaceutical/ pesticides outsourcing and contract research.
 

We are committed to provide excellence in researching, manufacturing and drug discovery process.
 

Our research team of scientists consists of western-trained Ph.D.s with experience and capabilities in drug R&D methodologies and medicinal chemistry.

 

Details:

PR-619 is a broad-range DUB inhibitor with potential for further development as a chemotherapeutic agent in cancer therapy.
IC50 Value: 3.93 μM (EC50, USP4); 7.2 μM (EC50, USP2 core); 5.10 μM (EC50, USP20) [1]
Target: DUBs
in vitro: PR-619 induces HCT116 cell death with EC50 values of 6.3 μM [1]. The general deubiquitylase (DUB) inhibitor, PR-619 attenuated KCa3.1 degradation, indicative of deubiquitylation being required for lysosomal delivery [2]. Proteasome inhibition by MG-132 and deubiquitinase inhibition by PR-619 induces significant changes to the ubiquitin landscape, but that not all ubiquitination sites regulated by MG-132 and PR-619 are likely substrates for the ubiquitin-proteasome system [3]. Cells were incubated with PR-619, a broad-range, reversible inhibitor of ubiquitin isopeptidases. Incubation with PR-619 led to morphological changes, the upregulation of heat shock proteins (HSP), including HSP70 and αB-crystallin, and to protein aggregates near the MTOC, containing ubiquitin, HSPs, and the ubiquitin binding protein p62, which may provide a link between the UPS and autophagy. Thus, inhibition of DUB activity caused stress responses and the formation of protein aggregates resembling pathological inclusions observed in aggregopathies [4].
in vivo:

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