Eeyarestatin I
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货号：A893133同义名：
Eeyarestatin 1
Eeyarestatin I 是一种有效的内质网相关蛋白降解 (ERAD) 抑制剂和蛋白质转运抑制剂。Eeyarestatin I 通过诱导 NOXA 蛋白介导的凋亡来防止蛋白质转运，并表现出抗癌活性。
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Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
Eeyarestatin I is a potent inhibitor of endoplasmic reticulum-associated protein degradation (ERAD) and a potent inhibitor of protein translocation. Eeyarestatin I inhibits the Sec61 translocon. Eeyarestatin I targets the process of p97-associated deubiquitination (PAD) and inhibits atx3-dependent deubiquitination. Eeyarestatin I interferes with a step prior to proteasomal degradation. Eeyarestatin I induces cell death via the pro-apoptotic protein NOXA and has anticancer effects[1][2][3][4][5].Acting in the 2.5-40 μM concentration range for 48 hours, Eeyarestatin I increases endoplasmic reticulum (ER) stress markers, including Bip and CHOP as low as 20 μM, and can lead to cell death in A549 and H358 cells in a dose-dependent manner and ubiquitylation of key proteins, including PERK and IRE1α[1].Eeyarestatin I prevents the transfer of nascent proteins from the membrane-targeting complex to the ER transporter machinery, most likely by inactivating the Sec61 complex[2].
Eeyarestatin I 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Human proximal tubular epithelial cells (HK-2)
10 μM
24 hours
To investigate the effect of EerI on TGF-β1-induced fibrosis in HK-2 cells. Results showed that EerI treatment reversed Klotho protein expression and ameliorated epithelial-mesenchymal transition (EMT).
Int J Med Sci. 2022 Jan 9;19(2):321-330
HeLa cells
10 μM
ES1 enhances Ca2+ leakage via Sec61 complexes, resulting in ER Ca2+ depletion
Cell Chem Biol. 2019 Apr 18;26(4):571-583. e6
HEK-D1ER cells
1-10 μM
4-17 minutes
ES1 interferes with cellular Ca2+ homeostasis by enhancing Sec61-mediated Ca2+ leakage, leading to ER Ca2+ depletion
Cell Chem Biol. 2019 Apr 18;26(4):571-583. e6
MIA PaCa-2 cells
2.5 μM
5 days
Assess cell viability and apoptosis, combined treatment significantly reduced cell viability and induced apoptosis
BMC Cancer. 2021 Mar 6;21(1):237
PANC-1 cells
2.5 μM
5 days
Assess cell viability and apoptosis, combined treatment significantly reduced cell viability and induced apoptosis
BMC Cancer. 2021 Mar 6;21(1):237
4292 cells
3 μM
5 days
Assess cell viability and apoptosis, combined treatment significantly reduced cell viability and induced apoptosis
BMC Cancer. 2021 Mar 6;21(1):237
Eeyarestatin I 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Male C57BL/6 mice
Unilateral ureteral obstruction (UUO)-induced renal interstitial fibrosis (RIF) model
Intraperitoneal injection
2.5 mg/kg
Once daily for 10 days
To investigate the effect of ERAD-specific inhibitor EerI on UUO-induced downregulation of Klotho protein expression. Results showed that EerI significantly increased Klotho protein expression, especially soluble (functional) Klotho, and attenuated kidney injury.
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