PYR-41

SKU: orb1300603

Description

PYR-41

Research Area

Cell Biology, Protein Biochemistry

Key Properties

• CAS Number: 418805-02-4
• MW: 371.3
• Purity: 98.25%
• Formula: C₁₇H₁₃N₃O₇
• SMILES: CCOC(=O)c1ccc(cc1)N1NC(=O)\C(=C\c2ccc(o2)[N+]([O-])=O)C1=O
• Target: E1/E2/E3 Enzyme,Apoptosis
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.69 mM);DMSO:5.5 mg/mL (14.81 mM)

Bioactivity

• Target IC50:
  E1:< 10 μM
• In Vitro:
  PYR-41 (50 μM) inhibits activity of ubiquitin-activating enzyme E1 by over 90%. PYR-41 could be a target for nucleophilic attack and potentially reacts with the active site cysteine of E1. PYR-41 efficiently blocks cyclin E degradation. PYR-41 decreases the level of E1fUb thioesters in cells with a IC50 of between 10 and 25 μM, and prevents proteasome inhibitor–induced accumulation of ubiquitylated proteins. PYR-41 increases total sumoylation in cells and in cell harboring temperature-sensitive E1. PYR-41 is able to inhibit both proteasome-dependent and proteasome-independent activities of ubiquitylation. PYR-41 (50 μM) attenuates 1 ng/mL IL-1α-mediated nuclear factor-κB activation by >60% through preventing the downstream ubiquitylation and proteasomal degradation of IκBα. PYR-41 inhibits degradation of p53 and activates the transcriptional activity of p53, which enable its differentially killing transformed p53-expressing cells. PYR-41 blocks ubiquitination reactions but paradoxically leads to the accumulation of high MW ubiquitinated proteins. PYR-41 also has equal or greater inhibitory activity against several deubiquitinases (DUBs) in intact cells and purified USP5 in vitro. PYR-41 also mediates cross-linking of specific protein kinases (Bcr-Abl, Jak2) to inhibit their signaling activity.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Apoptosis, E1 activating enzyme, E1 Enzyme, E1/E2/E3 Enzyme, E2 conjugating enzyme, E2 Enzyme, E1Enzyme, E3Enzyme, E3 ligating enzyme, E2Enzyme, E3 Enzyme, Inhibitor, inhibit, PYR41, PYR-41, PYR 41, Ubiquitin activating enzyme, Ubiquitin conjugating enzyme, Ubiquitin ligase, Ubiquitin-activating Enzyme E1

Compound Identifiers

PubChem CID

5335621