GLPBio

Eeyarestatin I

Catalog No.: GC13855Purity:>98.00%
COASDSData Sheet

مثبط لتحلل الغشاء الخلوي المرتبط بالشبكة الإندوبلازمية ونقل البروتين.

المنتجات مخصصة للاستخدام البحثي فقط، وليست للاستخدام البشري. نحن لا نبيع للمرضى.

Eeyarestatin I
Cas No.: 412960-54-4
5mgIn Stock
$87.00
1
10mgIn Stock
$162.00
1
25mgIn Stock
$312.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

المراجع (Citations)

لا تتوفر حاليًا مراجع لهذا المنتج. فيما يلي مجموعة مختارة من المنشورات التي تستشهد بمنتجات GlpBio.
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    Nature
    641, 529–536 (2025)
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    Cell
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الوصف (Description)

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.

البروتوكول (Protocol)

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:
[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]. 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.

وثائق المنتج (Product Documents)

Purity:>98.00%Appearance:A solid
COASDSData Sheet

الخصائص الكيميائية (Chemical Properties)

رقم CAS
412960-54-4
الاسم الكيميائي
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
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
الصيغة الجزيئية
C27H25Cl2N7O7
الوزن الجزيئي
630.44
الذوبانية
30mg/mL in DMSO or DMF
التخزين
Store at -20°C
إرشادات عامة
اختر مذيبًا مناسبًا وفقًا لبيانات ذوبانية المنتج. بعد التحضير، قسّم المحلول المخزون إلى أجزاء لتجنب دورات التجميد والذوبان المتكررة.
استخدم المحاليل المخزونة خلال 6 أشهر عند حفظها في -80°C، أو خلال شهر واحد عند حفظها في -20°C.
لتحسين الذوبانية، سخّن الأنبوب إلى 37°C وعرّضه للموجات فوق الصوتية لمدة مناسبة.
شروط الشحن
تُشحن عينات التقييم مع عبوات تبريد. وتُشحن الأحجام الأخرى المتاحة في درجة حرارة الغرفة، أو مع عبوات تبريد عند الطلب.

الحاسبات (Calculators)المولارية / التخفيف / الوزن الجزيئي / تحويل الوحدات / تركيبة داخل الجسم الحي / الذوبانية

g/mol

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