Key Specifications Table
|Empirical Formula||CAS #|
Pricing & Availability
An invalid quantity was specified. The product quantity has been adjusted.
|324521-25MG||Glass bottle||25 mg||
|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 (Kd = 5 - 10 µM) 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 µM 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 µM in A9 and 293T cultures). EerI culture treatment (10 µM) 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.|
|Synonyms||ES1, 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, EerI, ERAD Inhibitor II, p97 Inhibitor II, Valosin-containing Protein Inhibitor II, VCP Inhibitor II|
|Form||Light yellow-orange solid|
|Structure formula Image|
|Purity||≥90% by HPLC|
|Safety Information according to GHS|
|Product Usage Statements|
|Packaged under inert gas||Packaged under inert gas|
|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.