PYR-41

Chemical Compound
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PYR-41 is the first cell permeable inhibitor of ubiquitin-activating enzyme E1, irreversibly inhibits ubiquitin-activating enzyme activity.It is a pyrazone compound that showed little or no activity on E2, E3.<ref>

biological activity of PYR41 in selleckchem(link). {{{website}}}. selleck chemicals LLC. Sep 25, 2014.

</ref>
Unexpectedly, despite of ubiquitylation inhibition, PYR-41 also enhances total sumoylation in cells.<ref>,

 Protein cross-linking as a novel mechanism of action of a ubiquitin-activating enzyme inhibitor with anti-tumor activity., 
 Biochem Pharmacol, 
 
 Vol. 82(Issue: 4),
 pp. 341–349,
 DOI: 10.1016/j.bcp.2011.05.012,</ref>

PYR41 also blocks the downstream ubiquitination and ubiquitination-dependent protein degradation or other ubiquitination-mediated cellular activities. Besides, PYR-41 inhibits degradation of p53, a tumour suppressor and also activates the transcription activity of it.<ref>,

 Ubiquitin-activating enzyme E1 inhibitor PYR-41 attenuates angiotensin II-induced activation of dendritic cells via the IκBa/NF-κB and MKP1/ERK/STAT1 pathways., 
 Immunology, 
 
 Vol. 142(Issue: 2),
 pp. 307–319,
 DOI: 10.1111/imm.12255,
 
 PMC: 4008238,</ref> PYR-41 and related pyrazones selectively kill transformed p53 expressing cells, suggesting that E1 inhibitors may be potential therapeutics in cancer.

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