Molecular structure of Eeyarestatin I, CAS Number: 412960-54-4
Eeyarestatin I (CAS 412960-54-4)
See product citations (12)
Alternate Names:
3-(4-Chlorophenyl)-4-[[[(4-chlorophenyl)amino]carbonyl]hydroxyamino]-5,5-dimethyl-2-oxo-1-imidazolidineacetic acid 2-[3-(5-nitro-2-furanyl)-2-propen-1-ylidene]hydrazide
Application:
Eeyarestatin I is a potent inhibitor of endoplasmic reticulum associated protein degradation
CAS Number:
412960-54-4
Purity:
≥98%
Molecular Weight:
630.44
Molecular Formula:
C27H25Cl2N7O7
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
Eeyarestatin I (ESI) is an endoplasmic reticulum associated degradation (ERAD) inhibitor. This compound is found to suppress protein translocation and therefore limit the elimination of misfolded proteins from the endoplasmic reticulum. Studies suggest that Eeyarestatin I specifically targets a component of the Sec61 complex which forms the membrane pore of the ER translocon. Additional data shows the cytotoxicity characteristics of Eeyarestatin I which are caused by Bcl-2 homology3-only pro-apoptotic protein NOXA activation by Eeyarestatin I.
Eeyarestatin I (CAS 412960-54-4) References
- Dissection of the dislocation pathway for type I membrane proteins with a new small molecule inhibitor, eeyarestatin. | Fiebiger, E., et al. 2004. Mol Biol Cell. 15: 1635-46. PMID: 14767067
- Inhibition of p97-dependent protein degradation by Eeyarestatin I. | Wang, Q., et al. 2008. J Biol Chem. 283: 7445-54. PMID: 18199748
- ERAD inhibitors integrate ER stress with an epigenetic mechanism to activate BH3-only protein NOXA in cancer cells. | Wang, Q., et al. 2009. Proc Natl Acad Sci U S A. 106: 2200-5. PMID: 19164757
- Eeyarestatin I inhibits Sec61-mediated protein translocation at the endoplasmic reticulum. | Cross, BC., et al. 2009. J Cell Sci. 122: 4393-400. PMID: 19903691
- The ERAD inhibitor Eeyarestatin I is a bifunctional compound with a membrane-binding domain and a p97/VCP inhibitory group. | Wang, Q., et al. 2010. PLoS One. 5: e15479. PMID: 21124757
- Eeyarestatin 1 interferes with both retrograde and anterograde intracellular trafficking pathways. | Aletrari, MO., et al. 2011. PLoS One. 6: e22713. PMID: 21799938
- Inhibition of endoplasmic reticulum-associated degradation rescues native folding in loss of function protein misfolding diseases. | Wang, F., et al. 2011. J Biol Chem. 286: 43454-64. PMID: 22006919
- Inhibition of protein translocation at the endoplasmic reticulum promotes activation of the unfolded protein response. | McKibbin, C., et al. 2012. Biochem J. 442: 639-48. PMID: 22145777
- Regulation of VCP/p97 demonstrates the critical balance between cell death and epithelial-mesenchymal transition (EMT) downstream of ER stress. | Shah, PP. and Beverly, LJ. 2015. Oncotarget. 6: 17725-37. PMID: 25970786
- Chemical Modulation of Endocytic Sorting Augments Adeno-associated Viral Transduction. | Berry, GE. and Asokan, A. 2016. J Biol Chem. 291: 939-47. PMID: 26527686
- Eeyarestatin I derivatives with improved aqueous solubility. | Ding, R., et al. 2016. Bioorg Med Chem Lett. 26: 5177-5181. PMID: 27729187
- Eeyarestatin 24 impairs SecYEG-dependent protein trafficking and inhibits growth of clinically relevant pathogens. | Steenhuis, M., et al. 2021. Mol Microbiol. 115: 28-40. PMID: 32798330
- Self-complementarity in adeno-associated virus enhances transduction and gene expression in mouse cochlear tissues. | Casey, G., et al. 2020. PLoS One. 15: e0242599. PMID: 33227033
- Inhibition of ERAD synergizes with FTS to eradicate pancreatic cancer cells. | Du, R., et al. 2021. BMC Cancer. 21: 237. PMID: 33676427
- Eeyarestatin I, an inhibitor of the valosin-containing protein, exhibits potent virucidal activity against the flaviviruses. | Rodrigo, I., et al. 2022. Antiviral Res. 207: 105416. PMID: 36113629
Inhibitor of:
(eukaryotic translation initiation factor) eIF, (eukaryotic translation initiation factor) eIF1, (eukaryotic translation initiation factor) eIF2, (eukaryotic translation initiation factor) eIF5, α-tectorin, β-1,3-Gal-T1, 9030025P20Rik, A530082C11Rik, AGTPBP1, ARL6IP4, ASB-1, ASB-12, ASB-3, ASB-7, ATF-6α, BAP29, BNIP-1, CCDC47, CLN6, CLPTM1, CLPX, CPN reg, CREB3L1, CRELD2, CTAGE6, Derlin-3, DnaJC25, E4F1, EG229571, EG229862, EG667977, eIF2α, eIF4G, EMC (ER Membrane Protein Complex), eRF1, FAM134A_Fam134a, FAM158A, FBXW2, Gm71, GOLGA6L, GP78-1, HERPUD2, HLA-B, IBRDC1, KDEL ER Marker, KDEL receptor 2, KDEL receptor 3, KIAA0090, KLHL38, LAP1B, LPPR3, LRSAM1, Makorin-2, MCFD2, MGC29506, MIA2, mKIAA1530, MRCL3, MUT, Ndfip2, NgR2, NOB1P, OTUB2, PCIA1, PDIR, prefoldin 6, Psmg2, RECS1, Reticulon, RNF145, RNF44, scotin, SDF-2L1, SDF-4, SEC11A, SEC11C, SEC16S, SEC23A, Sec61, Sec61α1, Sec61γ, Sec62, Sec63, Sel-1L2, SIL1, SPCS2, SPP, SURF-4, Synoviolin, TAPBPL, TCP-1 ζ2, TM9SF2, TMCO4, TMEM233, TMTC4, TMX3, Torsin4A, TRAM2, TRIM44, TRIM6-TRIM34, TRIM64B, TXNDC16, UBAP2, UBE2QL1, UBL4A, UBQLNL, UBXD1, UBXD3, UBXD4, UFD1, UGGT1, USP41, VCP, VCPIP1, WRB, and ZFAND1.Activator of:
AUP1, Cdc34, CHP1, Derlin-1, Derlin-2, Derlin-3, DnaJB12, ENGase, ERdj4, ERp27, ERp29, ERp72, FAM18A, FAM62C, FBL2, FBL4, FBXO16, GP78-2, GRP 94, Herc4, HSPA14, Lunapark, MAN2A2, NEURL1B, PDI, RFT1, RHBDL2, Ribophorin I, RNF214, SEC23B, Sec31A, Sec61, Sec61α1, Sec61α2, Shigatoxin 1, TCP-1 β, TEX264, TMEM33, TMEM92, TRC8, tsg 101, TXNDC1, TXNDC13, UBE1L, UBE2J2, UBXN2B, and ZSWIM7.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Eeyarestatin I, 5 mg | sc-358130B | 5 mg | $112.00 | |||
Eeyarestatin I, 10 mg | sc-358130 | 10 mg | $199.00 | |||
Eeyarestatin I, 25 mg | sc-358130A | 25 mg | $347.00 | |||
Eeyarestatin I, 50 mg | sc-358130C | 50 mg | $683.00 | |||
Eeyarestatin I, 100 mg | sc-358130D | 100 mg | $1336.00 | |||
Eeyarestatin I, 500 mg | sc-358130E | 500 mg | $5722.00 |