"目录号: HY-15282
Metabolic Enzyme/ProteaseAutophagy-
E-64 是一种有效的不可逆的半胱氨酸蛋白酶 (cysteine proteases) 抑制剂，抑制papain，IC50为 9 nM。
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生物活性
Description
E-64 is a potent irreversible inhibitor against generalcysteine proteaseswithIC50of 9 nM forpapain.
IC50& Target
IC50: 9 nM (Papain)[1]
In Vitro
E-64 is a cathepsin B-specific inhibitor, and its binding modes with papain, actinidin, cathepsin L, and cathepsin K have been reviewed at the atomic level. E-64 has been widely used as a potent and irreversible (covalent-type) inhibitor for many cysteine proteases such as papain, ficin, actinidin, cathepsin B and L[1]. TheS.cerviadult parasites are incubated in the Kreb's Ringer bicarbonate (KRB) maintenance medium for 8 h at 37°C, 5% CO2with 5, 10, 20 and 40 μM concentration of E-64. E-64 shows a concentration and time dependent decrease in motility and viability of the parasites (EC50=16 μM)[2].
In Vivo
A broad spectrum of expression of CD4 and CD19 is found exists in both the islets and pancreatic lymph nodes (PLNs) and that anti-serpin B13 mAb exposure causes a significant shift that favored cells expressing low-to-intermediate amounts of these markers. However, this shift is abolished in animals that receive anti-serpin B13 mAb in the presence of the protease inhibitor E-64 (E64), which maintains its blocking activity under the experimental conditions used[3]. Dahl salt-sensitive (SS) rats are fed an 8% high salt NaCl diet and intravenously infused with the irreversible cysteine cathepsin inhibitor E-64 (1 mg/day) or the vehicle (control). Both the control and E-64 infused groups develope significant hypertension and kidney damage, and no difference of the mean arterial pressure and the hypertension-associated albuminuria is observed between the groups[4].
References
