PYR-41---Ubiquitin-activating Enzyme E1 Inhibitor


Catalog No. size PriceQuantity
M60201-2S 2 mg solid $79
M60201-10S 10mg solid $324

Description

Product Information
Molecular Weight: 371.30
Formula: C17H13N3O7
Purity: ≥98%
CAS#: 418805-02-4
Solubility: DMSO up to 100 mM
Chemical Name: (Z)-ethyl 4-(4-((5-nitrofuran-2-yl)methylene)-3,5-dioxopyrazolidin-1-yl)benzoate
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

Biological Activity:

 

PYR-41 is a specific and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 uM, with no or little activity against E2. It blocks ubiquitylation and prevents ubiquitin-mediated proteasomal degradation. It inhibits NF-κB activation, blocks degradation of p53, increases p21 levels and induces apoptosis in vitro. PYR-41 can also cause an increase in sumoylation of proteins.

 


How to Use:

 

 

  • In vitro: PYR-41 was used at 10-50 µM final concentration in various in vitro assays.
  • In vivo: n/a

 

 

 


Reference:

 

  1. Yang Y, et al. Inhibitors of ubiquitin-activating enzyme (E1), a new class of potential cancer therapeutics. (2007) Cancer Res. 67(19):9472-81.
  2. Kapuria V, et al. Protein cross-linking as a novel mechanism of action of a ubiquitin-activating enzyme inhibitor with anti-tumor activity. (2011) Biochem Pharmacol. 82(4):341-9.
  3. Ungermannova D, et al. Identification and mechanistic studies of a novel ubiquitin E1 inhibitor. (2012) J Biomol Screen. 17(4):421-34.




 

Products are for research use only. Not for human use.

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