Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal Name: 4-[4-[(5-nitro-2-furanyl)methylene]-3,5-dioxo-1-pyrazolidinyl]-benzoic acid, ethyl ester
Purity: ≥95% (mixture of cis and trans isomers)
Formula Markup: C17H13N3O7
Formula Weight: 371.3
CAS Number: 418805-02-4
Notes: PYR41 is an irreversible inhibitor of ubiquitin-activating enzyme (E1) with an IC50 value of less than 10 µM.{36793} PYR41 specifically inhibits ubiquitin-thioester bond formation (IC50 = 6.4 µM) and not adenylation.{34092} It is selective for E1 over ubiquitin-conjugating enzyme (E2) but does inhibit autoubiquitination of the HECT domain ubiquitin protein ligase (E3) Nedd4 at a concentration of 50 µM in an autoubiquitination assay.{36793} It inhibits proteasome-dependent and -independent ubiquitination and protein degradation when used at a concentration of 50 µM. PYR41 prevents activation of NF-κB, ubiquitination of TNF receptor-associated factor 6 (TRAF6), and proteasomal degradation of IκBα. It prevents degradation and induces transcriptional activity of the tumor suppressor p53 and preferentially induces apoptosis of E1A-transformed RPE cells expressing wild-type p53 over non-transformed RPE cells when used at concentrations ranging from 1 to 20 µM. PYR41 also increases net cellular sumoylation and irreversibly cross-links proteins such as JAK2 and Bcr-Abl.{36793,36794}
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