PYR 41|cas 418805-02-4| DC Chem|Supplier|Price|Buy  

PYR 41|cas 418805-02-4| DC Chem|Supplier|Price|Buy

DC Chemicals Supply: PYR 41|cas 418805-02-4,Purity: >98% ,Cat No. DC7257, In stock.

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PYR 41|cas 418805-02-4 ,Synonym: PYR41; PYR 41  ,Chemical name: Benzoicacid,4-[4-[(5-nitro-2-furanyl)methylene]-3,5-dioxo-1-pyrazolidinyl]-,ethylester ,Molecular Formula: C17H13N3O7 ,MW:371.3

PYR 41, cas 418805-02-4,Purity: >98%, Best Price and quality from DC Chemicals. 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 at E2.

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. [1] 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.[1]