EST

Bezeichnung:EST

CAS-Nr88321-09-9

Englisch Name:EST

CBNumberCB8228758

SummenformelC17H30N2O5

Molgewicht342.43

MOL-Datei88321-09-9.mol

EST physikalisch-chemischer Eigenschaften

Schmelzpunkt	126.2°C
Siedepunkt	477.88°C (rough estimate)
Dichte	1.0657 (rough estimate)
Brechungsindex	1.5800 (estimate)
storage temp.	-20°C
Löslichkeit	Soluble in DMSO, DMF or ethanol
pka	13.32±0.40(Predicted)
Aggregatzustand	White solid
Farbe	Fine needles from EtOH
Stabilität	Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.

Sicherheit

Kennzeichnung gefährlicher	Xi
R-Sätze:	36/37/38
S-Sätze:	26-36-24/25
RIDADR	3077
WGK Germany	2
RTECS-Nr.	RR0404300
HS Code	29242990
Toxizität	cyt-ham:lng 200 mg/L IYKEDH 17,815,86

Gefahreninformationscode (GHS)

EST Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
S-Sätze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
Beschreibung
E-64d is an irreversible, membrane-permeable inhibitor of lysosomal and cytosolic cysteine proteases and has diverse biological activities. It is a synthetic analog of E-64 and prodrug form of E-64c that inhibits calpain and the cysteine proteases cathepsins F, -K, -B, -H, and -L. E-64d (20-200 μM) induces cell cycle arrest at the G₂/M phase in A431 human epidermoid carcinoma cells. It inhibits protease-resistant prion protein accumulation in scrapie-infected neuroblastoma cells with an IC₅₀ value of 0.5 μM. E-46d also inhibits entry of vesicular stomatitis virus (VSV) particles pseudotyped with severe acute respiratory syndrome coronavirus (SARS-CoV) or SARS-CoV-2 spike glycoprotein into Vero cells, an effect that is reduced by expression of the serine protease TMPRSS2.
Verwenden
E-64d is an inhibitor of cathepsins B and L as well as a potential inhibitor of calpain. E-64d has been shown to inhibit lysosomal proteases. E-64d has been used in combination with Prepstatin A to interfere with autolysosomal digestion. E-64d displays neurovascular and neuronal protective effects after focal cerebral ischemia in rats.
Verwenden
E-64d has been used as a lysosomal inhibitor in human acute promyelocytic leukemia NB4 cells and Huh-7?cells. It has also been used as a protease inhibitor in free calcium physiological tyrode solution for perfusion into the isolated heart samples.
Definition
ChEBI: An L-leucine derivative that is the amide obtained by formal condensation of the carboxy group of (2S,3S)-3-(ethoxycarbonyl)oxirane-2-carboxylic acid with the amino group of N-(3-methylb tyl)-L-leucinamide.
Biochem/physiol Actions
E-64d is an epoxysuccinyl peptide and an inhibitor of cysteine protease cathepsin B, calpains 1 and 2. E-64d by its cathepsin B protease inhibition functionality, may serve as a potential drug for treating traumatic brain injury (TBI) and Alzheimer′s disease (AD). It inhibits gametocyte surface antigen resulting in a decreased oocyst production in Plasmodium falciparum.
Sicherheitsprofil
Moderately toxic by intraperitoneal route. An experimental teratogen. Experimental reproductive effects. Mutation data reported. Whenheated to decomposition it emits toxic fumes of NOx.
Lager
Store at -20°C
Einzelnachweise
1) McGowan?et al.?(1989),?Inhibition of calpain in intact platelets by the thiol protease inhibitor E-64d; Biochem. Biophys. Res. Commun.,?158?432 2) Wilcox and Mason (1992),?Inhibition of cysteine proteinases in lysosomes and whole cells; Biochem. J.,?285?495 3) Mizushima?et al.?(2010), Methods in mammalian autophagy research; Cell,?140?313

EST Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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