PYR 41

Bezeichnung:PYR 41

CAS-Nr418805-02-4

Englisch Name:PYR 41

CBNumberCB62535692

SummenformelC17H13N3O7

Molgewicht371.3

MOL-Datei418805-02-4.mol

PYR 41 physikalisch-chemischer Eigenschaften

Schmelzpunkt	228 - 235°C
Dichte	1.486±0.06 g/cm3(Predicted)
storage temp.	-20°C
Löslichkeit	Soluble in DMSO at 5mg/ml with warming
Aggregatzustand	powder
pka	7.43±0.20(Predicted)
Farbe	red to brown
Sensitive	Light Sensitive
Stabilität	Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 week.
InChIKey	ARGIPZKQJGFSGQ-LCYFTJDESA-N

Sicherheit

Kennzeichnung gefährlicher	Xn
R-Sätze:	22-43
S-Sätze:	36/37
WGK Germany	3

Gefahreninformationscode (GHS)

PYR 41 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Pyr41 (418805-02-4) inhibits ubiquitin activating enzyme E1 (>60% inhibition at 10 μM) with little or no activity against E2 or E3. Cell permeable
Verwenden
PYR 41 is an irreversible and cell-permeable UBE1 inhibitor.
Definition
ChEBI: 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 Actions
PYR-41 is a cell permeable inhibitor of Ubiquitin activating enzyme (E1) with little or no activity against E3, E2, or caspase enzymatic activity.
in vitro
in 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].
Lager
Store at -20°C
Einzelnachweise
1) 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 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

418805-02-4, PYR 41 Verwandte Suche:

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