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E-64d

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Chemical Structure| 88321-09-9 同义名 : E64c ethyl ester;Aloxistatin;ethyl ester Loxistatin;NSC 694281;Loxistatin;EST;EP 453
CAS号 : 88321-09-9
货号 : A162425
分子式 : C17H30N2O5
纯度 : 99%+
分子量 : 342.43
MDL号 : MFCD00132883
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(350.44 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 30 mg/mL(87.61 mM)，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
动物实验配方：

IP 2% DMSO+2% Tween80+40% PEG300+water 6 mg/mL clear

PO 0.5% CMC-Na 36 mg/mL suspension

生物活性
靶点

  • Cysteine Protease
描述 Cysteine proteases play multiple roles in basically all aspects of physiology and development. Furthermore, they are engaged in signalling pathways and in the response to biotic and abiotic stresses[3]. Aloxistatin is a specific and potent inhibitor of cysteine proteinases isolated from a culture of Aspergillus japonicus[3]. Aloxistatin at a series of concentrations was able to enter the intact platelet and inhibit the protease activity in lysed platelets when incubated for 5 min[4]. After a brief preincubation with the membrane-permeable, Aloxistatin (10 mg/ml) blunted PTH-induced (parathyroid hormone) cell proliferation in sub-confluent cultures and also attenuated proliferation and inhibited differentiation in longer-term confluent cultures[5]. Aloxistatin(100 mg/kg, p.o.) inhibited the activity of cathepsin B&L in skeletal muscle, heart, and liver of hamsters[6].
作用机制 Aloxistatin reacts irreversibly with the thiol group at the active site.
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
U937 cells Function assay Blockade of cathepsin G processing in human U937 cells by densitometry, IC50=1.1 μM 17535802
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.92mL

0.58mL

0.29mL

14.60mL

2.92mL

1.46mL

29.20mL

5.84mL

2.92mL
参考文献

[1]Wilkesman J. Cysteine Protease Zymography: Brief Review. Methods Mol Biol. 2017;1626:25-31. doi: 10.1007/978-1-4939-7111-4_3. PMID: 28608197.

[2]McGowan EB, Becker E, Detwiler TC. Inhibition of calpain in intact platelets by the thiol protease inhibitor E-64d. Biochem Biophys Res Commun. 1989 Jan 31;158(2):432-5. doi: 10.1016/s0006-291x(89)80065-8. PMID: 2537073.

[3]Murray EJ, Grisanti MS, Bentley GV, Murray SS. E64d, a membrane-permeable cysteine protease inhibitor, attenuates the effects of parathyroid hormone on osteoblasts in vitro. Metabolism. 1997 Sep;46(9):1090-4. doi: 10.1016/s0026-0495(97)90284-5. PMID: 9284902.

[4]Tamai M, Matsumoto K, Omura S, Koyama I, Ozawa Y, Hanada K. In vitro and in vivo inhibition of cysteine proteinases by EST, a new analog of E-64. J Pharmacobiodyn. 1986 Aug;9(8):672-7. doi: 10.1248/bpb1978.9.672. PMID: 3023601.