PYR-41

- Overview
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    Background
    
    Ubiquitylation is catalyzed by the sequential action of ubiquitinactivating enzyme (E1), a ubiquitin-conjugating enzyme (E2) and a ubiquitin protein ligase (E3). Ubiquitylation is essential to numerous cellular and developmental processes, including protein quality control, growth, apoptosis, antigen presentation, DNA repair, and signal transduction. PYR-41, 4[4-(5-nitro-furan-2-ylmethylene)-3,5-dioxo-pyrazolidin-1-yl]-benzoic acid ethyl ester, is a selective inhibitor of Ubiquitin-Activating Enzyme (E1).
    In vitro: In addition to blocking ubiquitylation, PYR-41 was found to increase total sumoylation in cells. PYR-41 could attenuate cytokine-mediated nuclear factor-KBactivation. This correlated with inhibition of nonproteasomal ubiquitylation of TRAF6, which is important to IKBkinase activation. PYR-41 also prevented the downstream ubiquitylation and proteasomal degradation of IKBA. Moreover, PYR-41 has demonstrated effective UAE E1 inhibition as well as some off-target inhibition of the other ubiquitin regulatory enzymes and signal-transducing proteins, suggesting it is a nonspecific inhibitor [1].
    In vivo: No animal in vivo data have been published so far.
    Clinical trial: Up to now, PYR-41 is still in the preclinical development stage.
- Properties
  - Alternative Name
    
    ethyl 4-[(4Z)-4-[(5-nitrofuran-2-yl)methylidene]-3,5-dioxopyrazolidin-1-yl]benzoate
    
    CAS Number
    
    418805-02-4
    
    Molecular Formula
    
    C17H13N3O7
    
    Molecular Weight
    
    371.3
    
    Appearance
    
    A solid
    
    Purity
    
    97.66%
    
    Solubility
    
    insoluble in H2O; ≥0.57 mg/mL in EtOH with ultrasonic; ≥18.55 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Lee MJ, Miller Z, et al. "H727 cells are inherently resistant to the proteasome inhibitor carfilzomib, yet require proteasome activity for cell survival and growth." Sci Rep. 2019 Mar 11;9(1):4089. PMID:30858500
    2. Susman MW, Karuna EP, et al. "Kinesin superfamily protein Kif26b links Wnt5a-Ror signaling to the control of cell and tissue behaviors in vertebrates." Elife. 2017 Sep 8;6. pii: e26509. PMID:28885975

PYR-41

Background

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