An irreversible inhibitor of ubiquitin-activating enzyme (E1; IC50 = 50 = 6.4 µM); selective for E1 over E2 but does inhibit autoubiquitination of the HECT domain E3 Nedd4 at 50 µM; inhibits proteasome-dependent and -independent ubiquitination and protein degradation at 50 µM; preferentially induces apoptosis of E1A-transformed RPE cells expressing wild-type p53 over non-transformed RPE cells at 1-20 µM; also increases net cellular sumoylation and irreversibly cross-links proteins such as JAK2 and Bcr-Abl

PYR41 – 5 mg

Brand:
Cayman
CAS:
418805-02-4
Storage:
-20
UN-No:
Non-Hazardous - /

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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Description

An irreversible inhibitor of ubiquitin-activating enzyme (E1; IC50 = 50 = 6.4 µM); selective for E1 over E2 but does inhibit autoubiquitination of the HECT domain E3 Nedd4 at 50 µM; inhibits proteasome-dependent and -independent ubiquitination and protein degradation at 50 µM; preferentially induces apoptosis of E1A-transformed RPE cells expressing wild-type p53 over non-transformed RPE cells at 1-20 µM; also increases net cellular sumoylation and irreversibly cross-links proteins such as JAK2 and Bcr-Abl

Formal name: 4-[4-[(5-nitro-2-furanyl)methylene]-3,5-dioxo-1-pyrazolidinyl]-benzoic acid, ethyl ester

Synonyms: 

Molecular weight: 371.3

CAS: 418805-02-4

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Product Type|Biochemicals|Small Molecule Inhibitors|Ubiquitin Ligase System||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|NF-κB Signaling||Research Area|Cancer|Cell Signaling|p53 Signaling||Research Area|Cancer|Transcription Factors|NF-κB||Research Area|Cancer|Transcription Factors|p53||Research Area|Cell Biology|Proteolysis|Ubiquitin/Proteasome System||Research Area|Immunology & Inflammation

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