MilliporeSigma™ Calbiochem™ ERO1 Inhibitor II, EN460

Description

A cell-permeable thiol reactive enone (EN) compound that selectively interacts with the active-site cysteine of reduced, active form of ERO1α and inhibits its activity (IC₅₀

A cell-permeable thiol reactive enone (EN) compound that selectively interacts with the active-site cysteine of reduced, active form of ERO1α and inhibits its activity (IC₅₀ = 1.9μM). Also prevents ERO1 re-oxidation both in vitro and in mouse embryonic fibroblasts. Activates the unfolded protein response and protects ER-stressed 293T cells. Can inhibit ERO1α even in the presence of an excess amount of competing thiols. Can inhibit ERO1α even in the presence of an excess amount of competing thiols. EN460 binding to ERO1α is shown to promote the loss of flavin adenine dinucleotide (FAD) from the holoenzyme. Its inhibitory action appears to be irreversible, however addition of FAD and tris(hydroxypropyl)phosphine (Cat. No. 598250) can restore some enzyme activity.

Specifications

• Color: Red
• Description: 99% by HPLC
• Molecular Formula: C₂₂H₁₂ClF₃N₂O₄
• Formula Weight: 460.8g/mol
• Solubility: DMSO
• Content And Storage: Protect from light
• Form: Solid
• Quantity: 25 mg