PYR 41

PYR 41 Basic information
Product Name:PYR 41
Synonyms:PYR 41;4-[4-[(5-Nitro-2-furanyl)methylene]-3,5-dioxo-1-pyrazolidinyl]benzoic acid ethyl ester;Benzoic acid, 4-[4-[(5-nitro-2-furanyl)methylene]-3,5-dioxo-1-pyrazolidinyl]-, ethyl ester;4-[4-[(5-Nitro-2-furanyl)methylene]-3,5-dioxo-1-pyrazolidinyl]benzoic acid ethyl ester PYR 41;PYR 41 4-[4-[(5-Nitro-2-furanyl)methylene]-3,5-dioxo-1-pyrazolidinyl]benzoic acid ethyl ester;4[4-(5-Nitro-furan-2-ylmethylene)-3,5-dioxo-pyrazolidin-1-yl]-benzoic acid ethyl ester;PYR 41, >=98%;CS-1129
CAS:418805-02-4
MF:C17H13N3O7
MW:371.3
EINECS:
Product Categories:Inhibitors
Mol File:418805-02-4.mol
PYR 41 Structure
PYR 41 Chemical Properties
Melting point 228 - 235°C
density 1.486±0.06 g/cm3(Predicted)
storage temp. -20°C
solubility Soluble in DMSO at 5mg/ml with warming
form powder
pka7.43±0.20(Predicted)
color red to brown
Sensitive Light Sensitive
Stability:Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 week.
InChIKeyARGIPZKQJGFSGQ-LCYFTJDESA-N
Safety Information
Hazard Codes Xn
Risk Statements 22-43
Safety Statements 36/37
WGK Germany 3
MSDS Information
PYR 41 Usage And Synthesis
DescriptionPyr41 (418805-02-4) inhibits ubiquitin activating enzyme E1 (>60% inhibition at 10 μM) with little or no activity against E2 or E3. Cell permeable
UsesPYR 41 is an irreversible and cell-permeable UBE1 inhibitor.
DefinitionChEBI: PYR-41 is an ethyl ester resulting from the formal condensation of the carboxy group of 4-{4-[(5-nitrofuran-2-yl)methylidene]-3,5-dioxopyrazolidin-1-yl}benzoic acid with ethanol. It is an irreversible and cell-permeable inhibitor of ubiquitin-activating enzyme E1. It has a role as an EC 6.2.1.45 (E1 ubiquitin-activating enzyme) inhibitor and an antineoplastic agent. It is an ethyl ester, a member of furans, a C-nitro compound, a member of pyrazolidines and a benzoate ester.
Biochem/physiol ActionsPYR-41 is a cell permeable inhibitor of Ubiquitin activating enzyme (E1) with little or no activity against E3, E2, or caspase enzymatic activity.
in vitroin addition to blocking ubiquitylation, pyr-41 was found to increase total sumoylation in cells. pyr-41 could attenuate cytokine-mediated nuclear factor-kbactivation. this correlated with inhibition of nonproteasomal ubiquitylation of traf6, which is important to ikbkinase activation. pyr-41 also prevented the downstream ubiquitylation and proteasomal degradation of ikba. moreover, pyr-41 has demonstrated effective uae e1 inhibition as well as some off-target inhibition of the other ubiquitin regulatory enzymes and signal-transducing proteins, suggesting it is a nonspecific inhibitor [1].
storageStore at -20°C
References1) Yang et al. (2007), Inhibitors of Ubiquitin-Activating Enzyme (E1), a New Class of Potential Cancer Therapeutics; Cancer Res., 67 9472 2) Mi et al. (2009), Cancer Preventive isothiocyanates induce selective degradation of cellular alpha- and beta-tubulins by proteasomes; J. Biol. Chem., 284 17039 3) Maehama et al. (2014), Nucleolar Stress Induces Ubiquitination-independent Proteasomal Degradation of PICT1 Protein PYR41; J. Biol. Chem., 289 20802 [Focus Citation]
PYR 41 Preparation Products And Raw materials
Brefeldin A Nutlin-3 MG-132 LFM-A13 NSC697923 Degrasyn (WP1130) PR-619 TYRPHOSTIN AG 879 Geldanamycin Bortezomib

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