PR-619 [2645-32-1]

Catalog number: HY-13814_10mM
Brand: MedChem Express
Packing: 10 mM
Other sizes: 10 mg
50 mg
Price: € 138.00
Expected delivery time: 10 days

Product specifications for - PR-619 [2645-32-1]

Product group: Chemicals
Category: Other
CAS No.: 2645-32-1
Purity: >98%
Molecular Formula: C7H5N5S2
Molecular weight: 223.28
Datasheet: Datasheet
  Research Use Only
UNSPSC: 12352200
Scientific information: 
Scientific info: PR-619 is a broad-range DUB inhibitor with potential for further development as a chemotherapeutic agent in cancer therapy. IC50 Value: 3.93 uM (EC50, USP4), 7.2 uM (EC50, USP2 core), 5.10 uM (EC50, USP20) [1] Target: DUBs in vitro: PR-619 induces HCT116 cell death with EC50 values of 6.3 uM [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 alphaB-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:
Safety information: