E-64

E-64 is an irreversible and selective cysteine protease inhibitor with IC50 of 9 nM for papain. (In Vitro) :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) . (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 (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.

66701-25-5

E-64 | E 64 | E64

>98% (HPLC)

DMSO:71 mg/mL warmed (198.65 mM) ; Ethanol:<1 mg/mL (<1 mM) ; Water:11 mg/mL warmed (30.77 mM)

O=C ([C@@H]1[C@@H] (C (O) =O) O1) N[C@H] (C (NCCCCNC (N) =N) =O) CC (C) C

C15H27N5O5

357.41

Storage temperature: -20°C. Stability: ≥ 2 years

For research use only.