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PR-619

Cat. No. M2565
PR-619 Structure
Synonym:

2,6-Diamino-3,5-dithiocyanopyridine

Size Price Availability Quantity
10mg USD 75  USD75 In stock
50mg USD 235  USD235 In stock
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Quality Control & Documentation
Biological Activity

PR-619 is a non-selective, reversible inhibitor of the deubiquitinylating enzymes (DUBs) with EC50 of 1-20 μM.

Customer Product Validations & Biological Datas
Source Viruses (2017). Figure 1. PR-619
Method western blotting
Cell Lines HeLa cells
Concentrations 20 μM
Incubation Time 24 h
Results Densitometric analyses of the western blot data illustrate that the efficacy of Gag processing was reduced by about 2-fold in cells treated with P22077 or PR-619, whereas cells treated with the DI P5091 had wt level, indicating that certain DUB activities regulate late steps of HIV replication.
Chemical Information
Molecular Weight 223.28
Formula C7H5N5S2
CAS Number 2645-32-1
Solubility (25°C) DMSO 35 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Fu-Shun Hsu, et al. PR-619, a General Inhibitor of Deubiquitylating Enzymes, Diminishes Cisplatin Resistance in Urothelial Carcinoma Cells through the Suppression of c-Myc: An In Vitro and In Vivo Study

[2] Longhao Wang, et al. Inhibition of deubiquitination by PR-619 induces apoptosis and autophagy via ubi-protein aggregation-activated ER stress in oesophageal squamous cell carcinoma

[3] Xinxin Hu, et al. The small molecule inhibitor PR-619 protects retinal ganglion cells against glutamate excitotoxicity

[4] Ian G Cowell, et al. The Deubiquitinating Enzyme Inhibitor PR-619 is a Potent DNA Topoisomerase II Poison

[5] Kotaro Soji, et al. Deubiquitinase inhibitor PR-619 reduces Smad4 expression and suppresses renal fibrosis in mice with unilateral ureteral obstruction

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Keywords: PR-619, 2,6-Diamino-3,5-dithiocyanopyridine supplier, Deubiquitinase, inhibitors, activators

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