There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
E 64 is a potent, irreversible, selective and water-soluble cysteine protease inhibitor with IC50 values of 1.4, 2.5 and 4.1 nM for cathepsin K, L and S, respectively, as well as exhibited inhibitory effect on papain, calpain, cathepsin B and cathepsin H, but not serine proteases (except trypsin)[1][2][3]. E 64 had no effect on the serine proteinases at a concentration of 0.5 mM, but could inhibit the serine proteinases trypsin[3]. Treatment with E 64 combined with pepstatin A could increase LC3-II accumulation due to the endogenous FoxO1 required autophagy induced by stress stimuli (oxidative stress or serum starvation)[4]. Through inhibition of cathepsins (lysosomal proteases), E 64 is used as lysosomal protease inhibitor[4][5]. E 64 is a main component of commercial used proteasome cocktail.
作用机制
The epoxysuccinyl group of E-64 irreversibly binds with an active thiol group of cysteine proteases to form a thioether linkage.[6]
E-64/蛋白酶抑制剂E 64 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Caco-2 cells
24 µM
2 hours
To evaluate the inhibitory effect of E-64 on IIL invasion into Caco-2 cell monolayers, results showed that E-64 significantly inhibited IIL invasion.
Vet Res. 2022 Mar 7;53(1):19.
Bovine cartilage explants
10 µM
21 days
To assess the effect of E-64 on cartilage degradation under inflammatory stimulation, results showed that E-64 did not significantly inhibit GPDPLQ1237 release.
Sci Rep. 2019 Feb 28;9(1):3050.
Human embryonic kidney cells
10 µM
24 hours
E-64 inhibits cellular degradation processes.
Proc Natl Acad Sci U S A. 1988 Jan;85(1):146-50.
MDA-MB-231 breast cancer cells
0-50 µM
24 hours
E-64 treatment significantly increased the amount of active cathepsin S intracellularly while significantly reducing the amount of active cathepsin L.
Int J Biochem Cell Biol. 2016 Oct;79:199-208.
Mature human osteoclasts
5 µM
3-4 days
Inhibition of osteoclast-mediated bone and cartilage degradation, E-64 significantly inhibited CTX-I and C2M release
Arthritis Res Ther. 2018 Apr 10;20(1):67.
Human osteoclasts
5 µM
3–4 days
To assess the effect of E-64 on osteoclast-mediated cartilage degradation, results showed that E-64 inhibited 72.1% of GPDPLQ1237 release.
Sci Rep. 2019 Feb 28;9(1):3050.
E-64/蛋白酶抑制剂E 64 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Trichinella spiralis infection model
Oral
24 μM
Single dose, lasting 6 days
To evaluate the effect of E-64 on the infectivity, survival, and development of Trichinella spiralis larvae, results showed that E-64 significantly reduced the number of intestinal adult worms.
Vet Res. 2022 Mar 7;53(1):19.
Mice
C57BL/6 mouse model
Intraperitoneal injection
5 mg/kg
Once daily for 7 days
E-64 shows protective effects against tissue damage.
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