Keap1-Nrf2 Interaction Probe, ML334-Calbiochem

产品说明

一般描述

A cell-permeable tetrahydroisoquinoline derivative that acts as a direct, non-covalent inhibitor of Keap1 - Nrf2 (Kelch-like ECH-associated protein 1 - nuclear factor erythroid 2-related factor 2) protein - protein interaction (K_d = 1 µM) that causes the dissociation of Nrf2 from keap1 in the cytosol. Exhibits ARE-inducing activity (EC₅₀ = 18 µM in U2OS Keap1-Nrf2 functional assay) and promotes Nrf2 translocation to the nucleus (EC₅₀ = 12 µM). Has good solubility in aqueous buffers (>100 µM in phosphate buffered saline).
A cell-permeable tetrahydroisoquinoline derivative that acts as a direct, non-covalent inhibitor of Keap1 - Nrf2 (Kelch-like ECH-associated protein 1 - nuclear factor erythroid 2-related factor 2) protein - protein interaction (K_d = 1 µM) that causes the dissociation of Nrf2 from keap1 in the cytosol. Exhibits ARE-inducing activity (EC₅₀ = 18 µM in U2OS Keap1-Nrf2 functional assay) and promotes Nrf2 translocation to the nucleus (EC₅₀ = 12 µM). Has good solubility in aqueous buffers (>100 µM in phosphate buffered saline).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

生化/生理作用

Primary Target
Keap1–Nrf2
Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Hu, L., et al, 2013, Bioorg. Med. Chem. Lett.23, 3039.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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