Product Name:
PR-619CAS No.:
2645-32-1Cat.No.:HY-13814
Product Data Sheet
Cat. No.:
HY 13814MWt:
223.28Formula:
C7H5N5S2Purity :>98%
25°C:DMSO 45mg/mL;Water
<1
Solubility:Mechanisms:Biological Activity:
D i ti
Pathways:Others; Target:Deubiquitinase
Pathways:Cell Cycle/DNA Damage; Target:Deubiquitinase 25C: DMSO 45 mg/mL; Water <1mg/mL; Ethanol <1 mg/mL
Description:
IC50 Value: 3.93 μM (EC50, USP4); 7.2 μM (EC50, USP2 core); 5.10 μM (EC50, USP20) [1]PR-619 is a broad-range DUB inhibitor with potential for further development as a chemotherapeutic
agent in cancer therapy. 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-132and PR-619are likely substrates for the ubiquitin-
References:
[1]. Altun M, Kramer HB, Willems LI, Activity-based chemical proteomics accelerates inhibitor
development for deubiquitylating enzymes. Chem Biol. 2011 Nov 23;18(11):1401-12.[2]. Udeshi ND, Mani DR, Eisenhaure T, Methods for quantification of in vivo changes in protein 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 upregulat...ubiquitination following proteasome and deubiquitinase inhibition. Mol Cell Proteomics. 2012
May;11(5):148-59.[3]. Udeshi ND, Mani DR, Eisenhaure T, Methods for quantification of in vivo changes in protein ubiquitination following proteasome and deubiquitinase inhibition. Mol Cell Proteomics. 2012
May;11(5):148-59.[4]. Seiberlich V, Goldbaum O, Zhukareva V, The small molecule inhibitor PR-619 of
deubiquitinating enzymes affects the microtubule network and causes protein aggregate formation in neural cells: implications for neurodegenerative diseases. Biochim Biophys Acta. 2012 Nov;1823(1...
Caution: Not fully tested. For research purposes only
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