E-64

66701-25-5

C15H27N5O5

H2O : 36 mg/mL (100.72 mM; Need ultrasonic and warming); DMSO : 50 mg/mL (139.90 mM; Need ultrasonic)

Autophagy; Metabolic Enzyme/Protease

E-64 is a potent irreversible inhibitor against general cysteine proteases with IC₅₀ of 9 nM for papain. 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]. The S.cervi adult parasites are incubated in the Kreb's Ringer bicarbonate (KRB) maintenance medium for 8 h at 37C, 5% CO₂ with 5, 10, 20 and 40 uM concentration of E-64. E-64 shows a concentration and time dependent decrease in motility and viability of the parasites (EC₅₀=16 uM)^[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].