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PYR-41

Catalog No.: 16122793
Cas No.: 418805-02-4
Purity : 98% 
16122793 - PYR-41 | CAS 418805-02-4

Catalog number : 16122793

CAS number : 418805-02-4

分子式 : C17H13N3O7 

分子量 : 371.3 

Iupac 化学名称 : PYR-41 

Smile : CCOC(=O)c1ccc(cc1)N2C(=O)/C(=C\c3ccc(o3)[N+](=O)[O-])/C(=O)N2

InChiKey : ARGIPZKQJGFSGQ-LCYFTJDESA-N

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同义词N/A 
英文同义词N/A 
分子式C17H13N3O7 
分子量371.3 
外观crystalline solid 
纯度98% 
可溶性Soluble in DMSO 
存储3 years -20ºCpowder 
运输条件Shipped under ambient temperature as non-hazardous chemical. 
SmileCCOC(=O)c1ccc(cc1)N2C(=O)/C(=C\c3ccc(o3)[N+](=O)[O-])/C(=O)N2
InChiKeyARGIPZKQJGFSGQ-LCYFTJDESA-N
InChiInChI=1S/C17H13N3O7/c1-2-26-17(23)10-3-5-11(6-4-10)19-16(22)13(15(21)18-19)9-12-7-8-14(27-12)20(24)25/h3-9H,2H2,1H3,(H,18,21)/b13-9-
MDLMFCD01469983
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PYR-41 is the first cell-permeable inhibitor of ubiquitin-activating enzyme E1, with no activity at E2.PYR-41 (50 M) 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 M, and prevents proteasome inhibitorCinduced 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 M) attenuates 1 ng/mL IL-1-mediated nuclear factor-B activation by >60% through preventing the downstream ubiquitylation and proteasomal degradation of IB. PYR-41 inhibits degradation of p53 and activates the transcriptional activity of p53, which enable its differentially killing transformed p53-expressing cells 

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