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Merck - 324521-25MG - Eeyarestatin I | CAS 412960-54-4 | Calbiochem | 25MG

  • MFR SKU: 324521-25MG
  • ITEM #: 11574991
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ITEM #: 11574991
A cell-permeable oxo-imidazolidinyl-hydroxyurea that localizes to ER, where it interacts with AAA ATPase p97 via its nitrofuran-containing moiety, without exhibiting affinity toward Hsp70 / ATPase NSF
This listing is for 25 mg Glass bottle

Merck - 324521-25MG - Eeyarestatin I | CAS 412960-54-4 | Calbiochem | 25MG

  • Item #: 11574991
  • MFR SKU: 324521-25MG
Technical Specs
  • Overview A cell-permeable oxo-imidazolidinyl-hydroxyurea that preferentially localizes to ER, where it interacts with AAA (ATPase associated with diverse cellular activities) ATPase p97 ( K d = 5 - 10 µ M) via its nitrofuran-containing moiety, without exhibiting affinity toward Hsp70 or AAA ATPase NSF (N-methylmaleimide-sensitive factor). Evidence indicates that EerI cellular metabolite, but not EerI itself, is responsible for the inhibition of ER membrane translocon sec61 complex-mediated transfer of newly synthesized polypeptide, resulting in a blockage of ER-mediated posttranslational glycosylation and signal peptide removal (Effective conc. = 8 µ M in HepG2 and HeLa cultures). Ether independent or as a consequence of the early effect on sec61 complex, EerI culture treatment also induces a selective dissociation of an 180 kDa protein from the atx3-containing p97/VCP (Valosin-containing protein) complex and a blockage of the complex-associated deubiquitination of ERAD (ER-associated protein degradation) substrates in a reversible manner, resulting in an accumulation of polyubiquitinated proteins (Effective conc. = 10 µ M in A9 and 293T cultures). EerI culture treatment (10 µ M) is also demonstrated to selectively induce cytotoxicity in lymphoid cell lines, BJAB, HBL-2, JEKO-1, Jurkat, KMS-12, MINO, as well as primary leukemia cells from CLL (chronic lymphocytic leukemia) patients, but not PBMC from healthy donors, by upregulating the BH3-only pro-apoptotic protein NOXA in cancer cells via ATF3/4 activation and a downregulation of H2A ubiquitination. Unlike DBeQ (Cat. No. 506190 ), EeRI does not inhibit p97 ATPase activity.
  • Catalogue Number 324521
  • Brand Family Calbiochem®
  • Synonyms ES1, EerI, 1-(4-Chloro-phenyl)-3-(3-(4-chloro-phenyl)-5, 5-dimethyl-1-(3-(5-nitro-furan-2-yl)-allyldiene-hydrazinocarbonylmethyl)-2-oxo-imidazolidin-4-yl)-1-hydroxyl-urea, ERAD Inhibitor II, p97 Inhibitor II, Valosin-containing Protein Inhibitor II, VCP Inhibitor II
  • References Chou, T.F., et al. 2011. Proc. Natl. Acad. Sci. USA 108, 4834.
  • Wang. Q, et al. 2010. PLoS ONE 5, e15479.
  • Cross, B.C.S., et al. 2009. J. Cell. Sci. 122, 4393.
  • Wang, Q., et al. 2009. Proc. Natl. Acad. Sci. USA 106, 2200.
  • Wang, Q., et al. 2008. J. Biol. Chem. 283, 7445.
  • Fiebiger, E., et al. 2004. Mol. Biol. Cell 15, 1635.
  • CAS number 412960-54-4
  • Form Light yellow-orange solid
  • Hill Formula CHClNO
  • Chemical formula CHClNO
  • Structure formula Image
  • Quality Level MQ100
  • Purity ≥ 90% by HPLC
  • Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
  • Toxicity Standard Handling
  • Storage +2° C to +8° C
  • Protect from Light Protect from light
  • Do not freeze Ok to freeze
  • Special Instructions Following reconstitution, aliquot and freeze (-20° C). Stock solutions are stable for up to 3 months at -20° C.
  • Packaged under inert gas Packaged under inert gas
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