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PYR-41 - Revision history
2026-04-22T03:49:58Z
Revision history for this page on the wiki
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Prab at 00:56, 17 March 2025
2025-03-17T00:56:50Z
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<td colspan="2" style="background-color: #fff; color: #202122; text-align: center;">Revision as of 00:56, 17 March 2025</td>
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Prab
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Prab: CSV import
2025-02-11T01:26:41Z
<p>CSV import</p>
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<td colspan="2" style="background-color: #fff; color: #202122; text-align: center;">Revision as of 01:26, 11 February 2025</td>
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Prab
https://wikimd.com/index.php?title=PYR-41&diff=5227749&oldid=prev
Prab: CSV import
2024-02-22T23:26:26Z
<p>CSV import</p>
<p><b>New page</b></p><div>{{multiple issues|<br />
{{Orphan|date=September 2014}}<br />
{{technical|date=September 2014}}<br />
}}<br />
{{Chembox<br />
| Name = PYR-41<br />
| ImageFile =PYR-41.svg<br />
| ImageSize = <br />
| ImageAlt = <br />
| IUPACName = 4[4-(5-nitro-furan-2-ylmethylene)-3,5-dioxo-pyrazolidin-1-yl]-benzoic acid ethyl ester<br />
| OtherNames = <br />
|Section1={{Chembox Identifiers<br />
| CASNo = 418805-02-4<br />
| PubChem = 5335621<br />
| ChemSpiderID = 4492747<br />
| SMILES = CCOC(=O)C1=CC=C(C=C1)N2C(=O)/C(=C\C3=CC=C(O3)[N+](=O)[O-])/C(=O)N2 <br />
| StdInChI = 1S/C17H13N3O7/c1-2-26-17(23)10-3-5-11(6-4-10)19-16(22)13(15(21)18-19)9-12-7-8-14(27-12)20(24)25/h3-9H,2H2,1H3,(H,18,21)/b13-9-<br />
| StdInChIKey = ARGIPZKQJGFSGQ-LCYFTJDESA-N}}<br />
|Section2={{Chembox Properties<br />
| Formula = C<sub>17</sub>H<sub>13</sub>N<sub>3</sub>O<sub>7</sub><br />
| MolarMass = 371.3 g/mol<br />
| Appearance = <br />
| Density = 1.5±0.1 g/cm3<br />
| MeltingPt = <br />
| BoilingPt = <br />
| Solubility = }}<br />
|Section3={{Chembox Hazards<br />
| MainHazards = <br />
| FlashPt = <br />
| AutoignitionPt = }}<br />
}}<br />
'''PYR-41''' is the first cell permeable inhibitor of [[Ubiquitin-activating enzyme|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>{{cite web|url=http://www.selleckchem.com/products/pyr-41.html|title=biological activity of PYR41 in selleckchem|publisher=selleck chemicals LLC|date=Sep 25, 2014}}</ref><br /><br />
Unexpectedly, despite of ubiquitylation inhibition, PYR-41 also enhances total [[sumoylation]] in cells.<ref>{{cite journal|journal=Biochem Pharmacol|title=Protein cross-linking as a novel mechanism of action of a ubiquitin-activating enzyme inhibitor with anti-tumor activity. |vauthors=Kapuria V, Peterson LF, Showalter HD, etal |date=Aug 15, 2011|volume=82|issue=4|pages=341–349|doi=10.1016/j.bcp.2011.05.012|PMID=21621524}}</ref><br /><br />
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 [[p53 tumor suppressor|tumour suppressor]] and also activates the transcription activity of it.<ref>{{cite journal|journal=Immunology|title=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.|date=Jun 2014|volume=142|issue=2|pages=307–319|doi=10.1111/imm.12255 |vauthors=Chen C, etal |PMID=24456201|pmc=4008238}}</ref> PYR-41 and related pyrazones selectively kill transformed p53 expressing cells, suggesting that E1 inhibitors may be potential therapeutics in cancer.<br />
<br />
==References==<br />
{{reflist}}<br />
<br />
[[category:4-Aminobenzoate esters]]<br />
[[Category:Furans]]<br />
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<br />
{{antineoplastic-drug-stub}}<br />
{{dictionary-stub1}}</div>
Prab