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PR-619 CAS NO.2645-32-1
- FOB Price: USD: 1.00-1.00 /Gram Get Latest Price
- Min.Order: 100 Gram
- Payment Terms: L/C
- Available Specifications:
≥98.0%(100-500)Gram≥98.0%(1000-5000)Gram
- Product Details
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
- ProName: PR-619
- CasNo: 2645-32-1
- Molecular Formula: C7H5N5S2
- Appearance: white solid
- Application: CAS：2645-32-1； Small molecule inhibit...
- DeliveryTime: 3 months
- PackAge: 100g,500g,1kg,25kg/drum
- Port: shang hai
- ProductionCapacity: 1000 Gram/Month
- Purity: 98%
- Storage: Dry seal
- Transportation: shipping
- LimitNum: 100 Gram
Superiority
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: