Eeyarestatin I
目录号 : GC13855Eeyarestatin I是一种有效的内质网相关蛋白降解(ERAD)抑制剂，也是一种有效的蛋白质易位抑制剂。它扰乱内质网 (ER) 稳态，具有与硼替佐米相似的抗癌活性。Eeyarestatin I可抑制Sec61转运蛋白。
Cas No.:412960-54-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
Cell lines | Normal human epidermal keratinocytes cells |
Preparation Method | Confluent HepG2 cells were treated with Eeyarestatin I for 1 hour in culture before a 30-minute starvation in the presence of the compounds in methionine- and cystine-free medium supplemented with 2mM glutamine. Cells were then metabolically labelled in the presence of the eyarestatin I by incubation in starvation medium containing for 30 minutes. |
Reaction Conditions | 8μM; 1h |
Applications | Eeyarestatin I modulates protein processing at the ER of cultured mammalian cells, when cells were incubated with 8μM Eeyarestatin I , an almost complete loss of secretory glycoproteins in the media was observed. |
| Animal experiment [2]: | |
Animal models | Unilateral ureteral obstruction(UUO) model |
Preparation Method | Male C57BL/6 mice (20-25g, 8 weeks old) were free access to food and water in at light-, temperature- and humidity-controlled environment. All mice were subjected to either a sham or UUO operation and were assigned randomly to 4 groups as follows: sham, UUO, Eeyarestatin I treatment and UUO plus Eeyarestatin I treatment. UUO procedure was performed as previously described. Briefly, experimental animals were anesthetized generally, and the right ureter was double-ligated at two locations following abdominal incision. Consequently, the right ureter was cut between the two locations. Mice in sham group undergone identical UUO procedure but the ureteral was not obstructed or ligated. Eeyarestatin I, an ERAD inhibitor, was injected into abdominal cavity in UUO mice at a dosage of 2.5mg/kg, and repeated on day. All mice were sacrificed at day 10 after UUO operation. Serum and kidney samples were collected and processed properly for further analyses. |
Dosage form | 2.5mg/kg; ip, 10d |
Applications | Eeyarestatin I upregulates renal Klotho protein expression, as well as sKlotho levels , without significantly altering Klotho mRNA level. |
References: | |
Eeyarestatin I, a potent endoplasmic reticulum-associated protein degradation (ERAD) inhibitor, is a potent protein translocation inhibitor. It disturbs endoplasmic reticulum (ER) homeostasis and has anticancer activities resembling that of Bortezomib. Eeyarestatin I inhibits Sec61 translocon[1].
Eeyarestatin I (8μM; 1h) modulates protein processing at the ER of cultured mammalian cells, when cells were incubated with 8μM Eeyarestatin I, an almost complete loss of secretory glycoproteins in the media was observed[2]. Eeyarestatin I (0.2-5μM; 4h) abolishes both Zika virus and Usutu virus infectivity in a dose-and time-dependent manner, in agreement with an antiviral activity occurring directly upon the viral particles[3]. Eeyarestatin I (10μM; 24h) abrogates TGF-β1-triggered Klotho reduction in cultured HK-2 cells[4].
Eeyarestatin I (2.5mg/kg; ip, 10d) upregulates renal Klotho protein expression, as well as sKlotho levels , without significantly altering Klotho mRNA level[4]. Inhibition of Valosin-containing protein's function by Eeyarestatin I (50µg/each; sc; 2 times) reduces tumor growth in NSCLC-xenograft model[5].
References:
[1] Cross B C S, McKibbin C, Callan A C, et al. Eeyarestatin I inhibits Sec61-mediated protein translocation at the endoplasmic reticulum[J]. Journal of cell science, 2009, 122(23): 4393-4400.
[2]. Cross B C S, McKibbin C, Callan A C, et al. Eeyarestatin I inhibits Sec61-mediated protein translocation at the endoplasmic reticulum[J]. Journal of cell science, 2009, 122(23): 4393-4400.
[3]Rodrigo I, Ballesta C, Nunes E B, et al. Eeyarestatin I, an inhibitor of the valosin-containing protein, exhibits potent virucidal activity against the flaviviruses[J]. Antiviral Research, 2022, 207: 105416.
[4]. Li S S, Kong J W, Yu L X, et al. Abnormally decreased renal Klotho is linked to endoplasmic reticulum-associated degradation in mice[J]. International Journal of Medical Sciences, 2022, 19(2): 321.
[5].Valle C W, Min T, Bodas M, et al. Critical role of VCP/p97 in the pathogenesis and progression of non-small cell lung carcinoma[J]. PloS one, 2011, 6(12): e29073.
Eeyarestatin I是一种有效的内质网相关蛋白降解(ERAD)抑制剂，也是一种有效的蛋白质易位抑制剂。它扰乱内质网 (ER) 稳态，具有与硼替佐米相似的抗癌活性。Eeyarestatin I可抑制Sec61转运蛋白[1]。
Eeyarestatin I（8μM；1h）调节培养的哺乳动物细胞 ER 中的蛋白质加工，当细胞与8μM Eeyarestatin I一起孵育时，培养基中分泌糖蛋白几乎完全消失[2]。Eeyarestatin I（0.2-5μM；4h）以剂量和时间依赖性方式消除寨卡病毒和乌苏图病毒的传染性，这与直接发生在病毒颗粒上的抗病毒活性一致[3]。Eeyarestatin I（10μM；24h）可消除培养的HK-2细胞中TGF-β1引发的Klotho减少[4]。
Eeyarestatin I（2.5 mg/kg；ip；10d）可上调肾脏 Klotho 蛋白表达以及sKlotho水平，而不会显著改变Klotho mRNA水平[4]。Eeyarestatin I （50 µg/each；sc；2次) 抑制含缬氨酸蛋白功能，降低NSCLC异种移植模型中的肿瘤生长[5]。
| Cas No. | 412960-54-4 | SDF | |
| 化学名 | 3-(4-chlorophenyl)-1-((R)-3-(4-chlorophenyl)-5,5-dimethyl-1-(2-((E)-2-((Z)-3-(5-nitrofuran-2-yl)allylidene)hydrazinyl)-2-oxoethyl)-2-oxoimidazolidin-4-yl)-1-hydroxyurea | ||
| Canonical SMILES | ClC1=CC=C(C=C1)N2[C@@H](C(C)(C)N(CC(N/N=C/C=C\C3=CC=C([N+]([O-])=O)O3)=O)C2=O)N(C(NC(C=C4)=CC=C4Cl)=O)O | ||
| 分子式 | C27H25Cl2N7O7 | 分子量 | 630.44 |
| 溶解度 | 30mg/mL in DMSO or DMF | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.5862 mL | 7.931 mL | 15.8619 mL |
| 5 mM | 0.3172 mL | 1.5862 mL | 3.1724 mL |
| 10 mM | 0.1586 mL | 0.7931 mL | 1.5862 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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