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E-64

E-64是一种非可逆的、选择性的半胱氨酸蛋白酶抑制剂,同样也抑制木瓜蛋白酶、钙蛋白酶和cathepsins B、H,但不抑制丝氨酸蛋白酶或天冬氨酸蛋白酶。抑制木瓜蛋白酶的IC50为9nM。E-64 可在丝虫的寄生虫中诱导氧化应激和凋亡。

  • 货号:
    TK0508
  • 规格:
    2mg
    5mg
    10mg
    25mg
  • 价格:
    0.00

产品参数

CAS No. 66701-25-5
生物活性E-64 (Proteinase inhibitor E 64) is a potent irreversible inhibitor against general cysteine proteases with IC50 of 9 nM for papain.
分子式C15H27N5O5
分子量357.41
运输条件Room temperature in continental US; may vary elsewhere.
储存条件Powder, -20°C ,3 years
溶解性数据DMSO : 250 mg/mL (699.48 mM; Need ultrasonic),H2O : 12.5 mg/mL (34.97 mM; Need ultrasonic)
体内研究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 (Proteinase inhibitor E 64), which maintains its blocking activity under the experimental conditions used. 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.
体外研究E-64 (Proteinase inhibitor 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. The S.cervi adult parasites are incubated in the Kreb's Ringer bicarbonate (KRB) maintenance medium for 8 h at 37°C, 5% CO2 with 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).
纯度及产品资料98%