DUB Inhibitor, PR-619- CAS 2645-32-1

CAS No.: 2645-32-1

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DUB Inhibitor, PR-619,2645-32-1
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I002906
Synonyms:

(2,6-diamino-5-thiocyanatopyridin-3-yl) thiocyanate

Molecular Formula:

C₇H₅N₅S₂

Molecular Weight:223.28
IC50::3.93 μM (EC50, USP4); 7.2 μM (EC50, USP2 core); 5.10 μM (EC50, USP20) [1]
Description: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.
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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:

Chem Calculators

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