E1286

Eeyarestatin I

synthetic (organic), ≥98% (HPLC), ERAD inhibitor, powder

• Synonym(e): 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
• Empirische Formel (Hill-System): C₂₇H₂₅Cl₂N₇O₇
• CAS-Nummer: 412960-54-4
• Molekulargewicht: 630.44
• MDL number: MFCD00319108
• UNSPSC Code: 12352204
• NACRES: NA.77

Eigenschaften

• Produktname: Eeyarestatin I, ≥98% (HPLC)
• biological source: synthetic (organic)
• Quality Level: 200
• assay: ≥98% (HPLC)
• form: powder
• storage condition: desiccated
• solubility: DMSO: 5 mg/mL
• storage temp.: 2-8°C
• SMILES string: Clc1ccc(cc1)N2C(C(N(C2=O)CC(=O)NN=CC=Cc4[o]c(cc4)[N+](=O)[O-])(C)C)N(O)C(=O)Nc3ccc(cc3)Cl
• 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)
• InChI key: JTUXTPWYZXWOIB-UHFFFAOYSA-N

Beschreibung

Biochem/physiol Actions

Eeyarestatin I is a potent inhibitor of endoplasmic reticulum associated protein degradation (ERAD). Specifically targets the p97-associated deubiquinating process (PAD) and inhibits ataxin-3 (atx3)-dependent deubiquitination.

Eeyarestatin I is a potent inhibitor of endoplasmic reticulum associated protein degradation (ERAD). Specifically targets the p97-associated deubiquinating process (PAD) and inhibits ataxin-3 (atx3)-dependent deubiquitination. Also inhibits Sec61-mediated protein translocation at the ER. Displays cytotoxic activity preferentially against cancer cells; induces cell death via the proapoptotic protein NOXA.

Eeyarestatin I or Eer1 promotes transcriptional activation of the pro-apoptotic protein NOXA by inducing activation of the NOXA transcription factors ATF3 and ATF4 and by inhibiting the degradation of histone H2A by blocking its ubiquitination. [1]

Other Notes

This product is a mixture of E/Z imine isomers

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable