L-TRANS-3-CARBOXYOXIRAN-2-CARBONYL-L-LEUCYLAGMATINE
N-(trans-epoxysuccinyl)-L-leucine 4-guanidinobutylamide
CAS: 66701-25-5
Molecular Formula: C15H27N5O5
L-TRANS-3-CARBOXYOXIRAN-2-CARBONYL-L-LEUCYLAGMATINE - Names and Identifiers
L-TRANS-3-CARBOXYOXIRAN-2-CARBONYL-L-LEUCYLAGMATINE - Physico-chemical Properties
| Molecular Formula | C15H27N5O5 |
| Molar Mass | 357.41 |
| Density | 1.44±0.1 g/cm3(Predicted) |
| Melting Point | >170°C (dec.) |
| Water Solubility | Soluble in DMSO (25mg/ml), or water (20mg/ml) |
| Solubility | Soluble in DMSO and water. |
| Appearance | White powder. |
| Color | White or off-white |
| BRN | 1405664 |
| pKa | 3.16±0.40(Predicted) |
| Storage Condition | 2-8°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in 1 |
| Sensitive | Light Sensitive |
| Refractive Index | 1.617 |
| MDL | MFCD00080261 |
| Use | This product is for scientific research only and shall not be used for other purposes. |
| In vitro study | E-64 rapidly inhibited the cysteine proteases cathepsin B,H ,L, and papain, whereas it had no effect on serine proteases or metalloproteases. E-64, a specific inhibitor of cysteine proteases, effectively blocks ovarian cancer cell invasion in vitro. In addition, E-64 also exhibited in vitro antiparasitic activity against Giardia lamella decapsulation. E-64 improves the pre-implantation development of somatic cell nuclear transfer embryos, which shows another important effect of E-64. |
| In vivo study | E-64 caused a significant reduction in the number of spontaneous metastases in M5076 tumor mice and had no effect on the formation of experimental metastases. E-64 also showed antiparasitic activity against mice infected with Giardia lamellae. |
L-TRANS-3-CARBOXYOXIRAN-2-CARBONYL-L-LEUCYLAGMATINE - Risk and Safety
| Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. |
| WGK Germany | 3 |
| RTECS | RR0390000 |
| FLUKA BRAND F CODES | 10 |
| HS Code | 29252900 |
L-TRANS-3-CARBOXYOXIRAN-2-CARBONYL-L-LEUCYLAGMATINE - Introduction
E-64 is an irreversible, powerful, highly selective cysteine protease inhibitor. E-64 does not react with non-protease functional sulfur groups, such as L-lactate dehydrogenase or creatine kinase. E-64 like other cysteine protease inhibitors, such as leucopeptide and antipain, do not inhibit serine proteases (except trypsin). E-64 trans-epoxysuccinyl (active moiety) irreversibly binds to many active sulfhydryl groups of cysteine proteases, such as papain, kiwifruit enzyme (actinidase), cathepsin B,H, and L. E-64 is a very useful cysteine protease inhibitor for in vivo research, because it has specific inhibitory characteristics, it can penetrate into cells and tissues, and has low toxicity.
Last Update：2022-10-16 17:27:48
L-TRANS-3-CARBOXYOXIRAN-2-CARBONYL-L-LEUCYLAGMATINE - Reference Information
| biological activity | E-64 is a non-reversible, selective cysteine protease inhibitor, also inhibit papain, calpain and cathepsin B, H, but does not inhibit serine or aspartic proteases. The IC50 for inhibition of papain was 9nm. E-64 can induce oxidative stress and apoptosis in filarial parasites. |
| Target | Value |
| Cysteine protease (Cell-free assay) | 9 nM |
| Use | E-64 is an effective ligand for affinity purification of cysteine proteases. When coupled to a thiolated affinity matrix, binding is no longer irreversible, but retention of specificity |
Last Update：2024-04-09 21:04:16
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View History
L-TRANS-3-CARBOXYOXIRAN-2-CARBONYL-L-LEUCYLAGMATINE
MHED HYDROCHLORIDE
苯磺酸,2,4,5-三氯-,肼
Agrimory Extract
bis([1-ethyl(3-oxetanil)]methyl)ether
Pentitol, 1-deoxy-1-(3,4-dihydro-7,8-dimethyl-2,4-dioxobenzo[g]pteridin-10(2H)-yl)-
CDD
松二糖 D-TURANOS
2-[4-[1-(4,4-二甲基-5H-恶唑-2-基)-1-甲基-乙基]苯基]乙醇
2-羟基泽兰内酯
MHED HYDROCHLORIDE
苯磺酸,2,4,5-三氯-,肼
Agrimory Extract
bis([1-ethyl(3-oxetanil)]methyl)ether
Pentitol, 1-deoxy-1-(3,4-dihydro-7,8-dimethyl-2,4-dioxobenzo[g]pteridin-10(2H)-yl)-
CDD
松二糖 D-TURANOS
2-[4-[1-(4,4-二甲基-5H-恶唑-2-基)-1-甲基-乙基]苯基]乙醇
2-羟基泽兰内酯