Chemistry:PYR-41
From HandWiki
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| Preferred IUPAC name
Ethyl 4-{(4Z)-4-[(5-nitrofuran-2-yl)methylidene]-3,5-dioxopyrazolidin-1-yl}benzoate | |
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3D model (JSmol)
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PubChem CID
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| Properties | |
| C17H13N3O7 | |
| Molar mass | 371.3 g/mol |
| Density | 1.5±0.1 g/cm3 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). | |
| Infobox references | |
PYR-41 is a cell permeable irreversible inhibitor of ubiquitin-activating enzyme E1.[1] It was also reported to increase sumoylation in cells.[1][2]
PYR-41 also blocks the downstream ubiquitination and ubiquitination-dependent protein degradation or other ubiquitination-mediated cellular activities. In addition, PYR-41 inhibits degradation of p53, a tumour suppressor.[3]
References
- ↑ 1.0 1.1 Yang, Yili; Kitagaki, Jirouta; Dai, Ren-Ming; Tsai, Yien Che; Lorick, Kevin L.; Ludwig, Robert L.; Pierre, Shervon A.; Jensen, Jane P. et al. (1 October 2007). "Inhibitors of Ubiquitin-Activating Enzyme (E1), a New Class of Potential Cancer Therapeutics". Cancer Research 67 (19): 9472–9481. doi:10.1158/0008-5472.CAN-07-0568. PMID 17909057.
- ↑ "Protein cross-linking as a novel mechanism of action of a ubiquitin-activating enzyme inhibitor with anti-tumor activity.". Biochem Pharmacol 82 (4): 341–349. Aug 15, 2011. doi:10.1016/j.bcp.2011.05.012. PMID 21621524.
- ↑ "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 142 (2): 307–319. Jun 2014. doi:10.1111/imm.12255. PMID 24456201.
category:4-Aminobenzoate esters
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