PR-619 is a non-selective, reversible inhibitor of the deubiquitinylating enzymes (DUBs) with EC50 of 1-20 μM.
|Source||Viruses (2017). Figure 1. PR-619|
|Cell Lines||HeLa cells|
|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.|
|Solubility (25°C)||DMSO 35 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
 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
 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
 Xinxin Hu, et al. The small molecule inhibitor PR-619 protects retinal ganglion cells against glutamate excitotoxicity
 Ian G Cowell, et al. The Deubiquitinating Enzyme Inhibitor PR-619 is a Potent DNA Topoisomerase II Poison
 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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