PYR-41

SKU: orb1300603

Description

PYR-41

Research Area

Product Categories/Products/Small Molecules,Ubiquitination|||Apoptosis

Key Properties

• CAS Number: 418805-02-4
• MW: 371.3
• Purity: 99.24%
• Formula: C₁₇H₁₃N₃O₇
• SMILES: CCOC(=O)c1ccc(cc1)N1NC(=O)\C(=C\c2ccc(o2)[N+]([O-])=O)C1=O

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 wit the active site cysteine of E1. PYR-41 efficiently blocks cyclin E degradation. PYR-41 decrease 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 preventin the downstream ubiquitylation and proteasomal degradation of IκBα. PYR-41 inhibits degradation of p53 and activate 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Compound Identifiers

PubChem CID

5335621