Eeyarestatin I

• Description :

  Eeyarestatin I, a potent endoplasmic reticulum-associated protein degradation (ERAD) inhibitor, is a potent protein translocation inhibitor. Eeyarestatin I inhibits Sec61 translocon. Eeyarestatin I targets the p97-associated deubiquitinating process (PAD) and inhibits atx3-dependent deubiquitination. Eeyarestatin I interferes at a step prior to proteasomal degradation. Eeyarestatin I induces cell death via the proapoptotic protein NOXA and has anticancer effects[1][2][3][4][5].

• UNSPSC :

  12352005

• Target :

  Apoptosis; p97

• Type :

  Reference compound

• Related Pathways :

  Apoptosis; Cell Cycle/DNA Damage

• Applications :

  Cancer-programmed cell death

• Field of Research :

  Cancer

• Assay Protocol :

  https://www.medchemexpress.com/eeyarestatin-i.html

• Purity :

  99.56

• Solubility :

  DMSO : 25 mg/mL (ultrasonic)

• Smiles :

  ON(C(C1(C)C)N(C(C=C2)=CC=C2Cl)C(N1CC(N/N=C/C=C/C(O3)=CC=C3[N+]([O-])=O)=O)=O)C(NC(C=C4)=CC=C4Cl)=O

• Molecular Formula :

  C27H25Cl2N7O7

• Molecular Weight :

  630.44

• References & Citations :

  [1]Parag P Shah, et al. Regulation of VCP/p97 demonstrates the critical balance between cell death and epithelial-mesenchymal transition (EMT) downstream of ER stress. Oncotarget. 2015 Jul 10;6 (19) :17725-37.|[2]Benedict C S Cross, et al. Eeyarestatin I inhibits Sec61-mediated protein translocation at the endoplasmic reticulum. J Cell Sci. 2009 Dec 1;122 (Pt 23) :4393-400.|[3]Qiuyan Wang, et al. Inhibition of p97-dependent protein degradation by Eeyarestatin I. J Biol Chem. 2008 Mar 21;283 (12) :7445-54.|[4]Qiuyan Wang, et al. ERAD inhibitors integrate ER stress with an epigenetic mechanism to activate BH3-only protein NOXA in cancer cells. Proc Natl Acad Sci U S A. 2009 Feb 17;106 (7) :2200-5.|[5]Pauwels E, et al. Inhibitors of the Sec61 Complex and Novel High Throughput Screening Strategies to Target the Protein Translocation Pathway. Int J Mol Sci. 2021 Nov 5;22 (21) :12007.

• Shipping Conditions :

  Blue Ice

• Storage Conditions :

  -20°C (Powder, sealed storage, away from moisture)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• CAS Number :

  [412960-54-4]