Description
Eeyarestatin I, a potent endoplasmic reticulum-associated protein degradation (ERAD) inhibitor, is a potent protein translocation inhibitor. Eeyarestatin I targets the p97-associated deubiquitinating process (PAD) and inhibits atx3-dependent deubiquitination. Eeyarestatin I induces cell death via the proapoptotic protein NOXA and has anticancer effects.
Product information
CAS Number: 412960-54-4
Molecular Weight: 630.44
Formula: C27H25Cl2N7O7
Chemical Name: 1-(4-chlorophenyl)-3-[3-(4-chlorophenyl)-5,5-dimethyl-1-({N'-[3-(5-nitrofuran-2-yl)prop-2-en-1-ylidene]hydrazinecarbonyl}methyl)-2-oxoimidazolidin-4-yl]-3-hydroxyurea
Smiles: CC1(C)C(N(O)C(=O)NC2C=CC(Cl)=CC=2)N(C2=CC=C(Cl)C=C2)C(=O)N1CC(=O)NN=CC=CC1=CC=C(O1)[N+]([O-])=O
InChiKey: JTUXTPWYZXWOIB-LWWHHIEBSA-N
InChi: InChI=1S/C27H25Cl2N7O7/c1-27(2)24(35(40)25(38)31-19-9-5-17(28)6-10-19)34(20-11-7-18(29)8-12-20)26(39)33(27)16-22(37)32-30-15-3-4-21-13-14-23(43-21)36(41)42/h3-15,24,40H,16H2,1-2H3,(H,31,38)(H,32,37)/b4-3+,30-15+
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Eeyarestatin I (2.5-40 μM; 48 hours; A549 and H358 cells) treatment causes a dose-dependent cell death of both A549 and H358 cells. Eeyarestatin I (2.5-40 μM; 48 hours; A549 and H358 cells) treatment increases endoplasmic reticulum (ER) stress markers including Bip and CHOP as low as 20 μM. Eeyarestatin I treatment shows a dose dependent ubiquitination of key proteins including PERK and IRE1α. Eeyarestatin I (20 μM; 48 hours; A549 and H358 cells) treatment induces cell migration and cell invasion. Eeyarestatin 1 prevents the transfer of nascent proteins from the membrane-targeting complex to the ER translocation machinery, most probably by inactivating the Sec61 complex.
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