EST

Product Name: EST
CAS No.: 88321-09-9
Chemical Name: EST
Synonyms: EST;ep453;E-64D;Estate;CS-1622;oxistatin;NSC694281;E64d,E-64d;LOXASTATIN;LOXISTATIN
CBNumber: CB8228758
Molecular Formula: C17H30N2O5
Formula Weight: 342.43
MOL File: 88321-09-9.mol

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EST Property

Melting point:: 126.2°C
Boiling point:: 477.88°C (rough estimate)
Density: 1.0657 (rough estimate)
refractive index: 1.5800 (estimate)
storage temp.: -20°C
solubility: Soluble in DMSO, DMF or ethanol
pka: 13.32±0.40(Predicted)
form: White solid
color: Fine needles from EtOH
Stability:: 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.

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Safety

Hazard Codes: Xi
Risk Statements: 36/37/38
Safety Statements: 26-36-24/25
RIDADR: 3077
WGK Germany: 2
RTECS: RR0404300
HS Code: 29242990
Toxicity: cyt-ham:lng 200 mg/L IYKEDH 17,815,86

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P405Store locked up.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: E8640
Product name: E-64d
Purity: protease inhibitor
Packaging: 250μg
Price: $144
Updated: 2024/03/01

Sigma-Aldrich

Product number: E8640
Product name: E-64d
Purity: protease inhibitor
Packaging: 1mg
Price: $385
Updated: 2024/03/01

Sigma-Aldrich

Product number: C1370
Product name: COT (30-397), active, GST tagged human
Purity: PRECISIO? Kinase, recombinant, expressed in baculovirus infected Sf9 cells, ≥70% (SDS-PAGE), buffered aqueous glycerol solution
Packaging: 10μg
Price: $524
Updated: 2024/03/01

Sigma-Aldrich

Product number: 330005
Product name: EST
Purity: A cell-permeable, irreversible inhibitor of cysteine proteases.
Packaging: 1mg
Price: $187
Updated: 2024/03/01

TCI Chemical

Product number: E1337
Product name: E-64d [for Biochemical Research]
Packaging: 5MG
Price: $101
Updated: 2024/03/01

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EST Chemical Properties,Usage,Production

Description

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.

Uses

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.

Uses

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.

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.

Safety Profile

Moderately toxic by intraperitoneal route. An experimental teratogen. Experimental reproductive effects. Mutation data reported. Whenheated to decomposition it emits toxic fumes of NOx.

storage

Store at -20°C

References

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 Preparation Products And Raw materials

Raw materials

Preparation Products

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EST Suppliers

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View Lastest Price from EST manufacturers

Career Henan Chemical Co

Product: EST 88321-09-9
Price: US $7.00/KG
Min. Order: 1KG
Purity: 99%
Supply Ability: 100KG
Release date: 2019-07-12

Career Henan Chemical Co

Product: EST 88321-09-9
Price: US $7.00/KG
Min. Order: 1KG
Purity: 99%
Supply Ability: 100KG
Release date: 2019-07-09

88321-09-9, ESTRelated Search:

GLYCIDAMIDE (S)-(+)-Methyl glycidyl ether EST (S)-(+)-4-AMINO-3-HYDROXYBUTANOIC ACID 2-Hydroxy-4-amino butanoic acid NALPHA-9-Fluorenylmethoxycarbonyl-S-trityl-L-cysteine pentafluorophenyl est 2,2'-[[4-[(3,5-dinitro-2-thienyl)azo]phenyl]imino]bis-ethano diacetate (est (R)-(-)-3-HYDROXY-2-METHYLPROPIONIC*ACID METHYL EST Isothiocyanic acid isobutyl est n-[3-(acetylamino)phenyl]-n-(3-methoxy-3-oxopropyl)-beta-alanin methyl est 1,2-CYCLOHEXANEDICARBOXYLICACID,BIS(2,3-EPOXYPROPYL)EST. 1,2,3,4,4a,4b,5, 6,7,9,10,10a-dodecahydro-1,4a-dimethyl-7- (1-methylethyl)-, 1,2,3-propanetriyl est1-Phenanthrenecarboxylic acid 8-FLUORO-5,6-DIHYDRO-5-METHYL-6-OXO-4H-IMIDAZO[1,5-A][1,4]BENZODIAZEPINE-3-CARBOXYLIC ACID ETHYL EST ETHYL (2S)-2,3-EPOXYPROPANOATE 2(2-HYDROXYETHOXY)ACETAMIDE ETHYL 2,3-EPOXYPROPANOATE (2-AMINO-ETHOXY)-ACETIC ACID Loxistatin acid

(2S,3S)-3-[[[(1S)-3-Methyl-1-[[(3-Methylbutyl)aMino]carbonyl]butyl]aMino]carbonyl]-2-oxiranecarboxylic acid ethyl ester

(2S,3S)-trans-Epoxysuccinyl-L-leucylaMido-3-Methylbutane ethyl ester, EST

(2S,3S)-ethyl 3-(((S)-1-(isopentylaMino)-4-Methyl-1-oxopentan-2-yl)carbaMoyl)oxirane-2-carboxylate

E-64-D(LOXISTATINE)

Estate

oxistatin

E64d,E-64d

E-64(Trans-Epoxysuccinyl-L-Leucylamido-(4-Guanidino)Butane)

L-trans-Epoxysuccinyl(OEt)-Leu-3-methylbuty

trans-epoxysuccinyl-L-leucylamido 3-methylbutane ethyl

EST, (2S,3S)-trans-Epoxysuccinyl-L-leucylamido-3-methylbutane ethyl ester

(2S,3S)-trans-epoxysuccinyl-L-*leucylamido-3-meth

aloxistatin

(2S)-3β-[[[(S)-3-Methyl-1-[[(3-methylbutyl)amino]carbonyl]butyl]amino]carbonyl]oxirane-2α-carboxylic acid ethyl ester

[2S,3S,(+)]-3β-[(S)-3-Methyl-1-(3-methylbutylcarbamoyl)butylcarbamoyl]-2α-oxiranecarboxylic acid ethyl ester

Aloxistatin (E-64d) EST Loxistatin

Aloxistatin (E64d

Aloxistatin(E-64d)

E64c ethyl ester)

E-64d, L-trans-Epoxysuccinyl(OEt)-Leu-3-MethylbutylaMide, EP453, Aloxistatin, Loxistatin

Aloxistatin, 98%, irreversible cell-permeable cysteine protease inhibitor

E-64d [for Biochemical Research]

ep453

ethylester,(2s-(2-alpha,3-beta(r*)))-mino)carbonyl)

(2S,3S)-ETHYL-TRANS-EPOXYSUCCINYL-L-LEUCYLAMIDO-3-METHYLBUTANE

(2S,3S)-TRANS-EPOXYSUCCINYL-L-LEUCYLAMIDO-3-METHYLBUTANE ETHYL ESTER

3-[[[(1S)-3-methyl-1[[(3S-methylbutyl)amino]carbonyl]butyl]amino]carbonyl]-2S-oxiranecarboxylic acid, ethyl ester

COT (30-397), active, GST tagged human

2-Oxiranecarboxylicacid,3-[[[(1S)-3-methyl-1-[[(3-methylbutyl)amino]carbonyl]butyl]amino]carbonyl]-,ethyl ester, (2S,3S)-

E 64d (Aloxistatin)

(2S,3S)-3-[[[(1S)-3-Methyl-1-[[(3-methylbutyl)amino]carbonyl]-butyl]amino]carbonyl]-2-oxiranec

L-TRANS-EPOXYSUCCINYL-LEU-3-METHYLBUTYLAMIDE-ETHYL ESTER

L-TRANS-EPOXYSUCCINYL(OET)-LEU-3-METHYLBUTYLAMIDE

LOXASTATIN

LOXISTATIN

(L-3TRANS-ETHOXYCARBONYLOXIRANE-2-CARBONYL)-L-LEUCINE-(3-METHYLBUTYL)AMIDE

EST

E-64D

EST - CAS 88321-09-9 - Calbiochem

CS-1622

ALOXISTATIN;E64D;E 64D;LOXISTATIN;E-64C ETHYL ESTER;EP 453;NSC 694281;NSC694281;NSC-694281

NSC 694281

NSC694281

NSC-694281

(2S,3S)-3-[[(2S)-4-Methyl-1-[(3-methylbutyl)amino]-1-oxo-2-pentanyl]carbamoyl]-2-oxiranecarboxylic Acid Ethyl Ester

Ethyl (2S,3S)-3-[[(2S)-4-Methyl-1-[(3-methylbutyl)amino]-1-oxo-2-pentanyl]carbamoyl]-2-oxiranecarboxylate

Aloxistatin (Loxistatin

E64d, NSC-694281)

Ethyl (2S,3S)-3-(((S)-1-(isopentylamino)-4-methyl-1-oxopentan-2-yl)carbamoyl)oxirane-2-carboxylate

88321-09-9

C17H30N2O5

Enzymes, Inhibitors, and Substrates

Enzyme Inhibitors by Enzyme

Enzyme Inhibitors

A to C

Calpain

BioChemical

Biochemicals and Reagents