Drug intelligence / Profile preview

PYR-41

Development stage
Discontinued
Modality
Small Molecules
Administration
Intravenous, Topical
01

Overview

PYR-41 is a cell-permeable, small molecule research compound that functions as a potent and irreversible inhibitor of the ubiquitin-activating enzyme E1 (UBA1). By targeting the initial step of the ubiquitin-proteasome system (UPS), PYR-41 prevents the ubiquitination of proteins, which in turn blocks their degradation by the proteasome. This inhibition results in the stabilization of key regulatory proteins, such as the tumor suppressor p53, and the suppression of NF-κB activation. While PYR-41 has demonstrated the ability to induce apoptosis and exhibit anti-tumor effects in various laboratory models, it is exclusively used as a pharmacological tool for research purposes and is not currently being developed for clinical use in humans.

Other names
4-[4-[(5-Nitro-2-furanyl)methylene]-3,5-dioxo-1-pyrazolidinyl]benzoic acid ethyl ester
02

Targets

UBA1

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