货号:A162425 同义名: E64c ethyl ester;Aloxistatin
E-64d(E64d)是一种细胞可渗透、不可逆的广谱半胱氨酸蛋白酶抑制剂,对MERS-CoV具有入侵阻断作用。
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产品名称 | Cysteine Protease ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Z-FA-FMK | ✔ | 99%+ | |||||||||||||||||
Leupeptin hemisulfate | ✔ | 97% | |||||||||||||||||
PMSF | ✔ | 95% | |||||||||||||||||
PD 151746 |
+
m-calpain, IC50: 5.33 μM μ-Calpain, IC50: 260 nM |
98% | |||||||||||||||||
Odanacatib |
++++
Cathepsin K (rabbit), IC50: 1 nM Cathepsin K (human), IC50: 0.2 nM |
99%+ | |||||||||||||||||
E-64 |
+++
Cysteine protease, IC50: 9 nM |
99%+ | |||||||||||||||||
E 64c | ✔ | 95% | |||||||||||||||||
E-64d | ✔ | 99%+ | |||||||||||||||||
MG-101 | ✔ | 98%+ | |||||||||||||||||
Calpeptin |
++
Calpain II (porcine kidney), ID50: 40 nM Calpain I (porcine erythrocytes), ID50: 52 nM |
98%+ | |||||||||||||||||
Cathepsin inhibitor 1 |
+++
Cathepsin L2, pIC50: 5.5 Cathepsin L, pIC50: 7.9 |
98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
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 |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 88321-09-9 |
分子式 | C17H30N2O5 |
分子量 | 342.43 |
别名 | E64c ethyl ester;Aloxistatin;ethyl ester Loxistatin;NSC 694281;Loxistatin;EST;EP 453 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Store in freezer, under -20°C |
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 |