(-)-DHMEQ (Dehydroxymethylepoxyquinomicin)

(-)-DHMEQ (Dehydroxymethylepoxyquinomicin) (Dehydroxymethylepoxyquinomicin) 是一种有效、选择性和不可逆的 NF-κB 抑制剂，可与半胱氨酸残基共价结合。

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Background

(-)-DHMEQ is a potent NF-κB inhibitor.

(-)-DHMEQ binds to cysteine 38 of RelA and cysteine 144 of RelB. (-)-DHMEQ at concentrations greater than 25 µM inhibits the LTβ-induced nuclear translocation of FLAG-RelB WT, whereas the inhibitory effect of (-)-DHMEQ on the nuclear translocation of FLAG-RelB (C144S) became weaker at the same concentrations[1].

[1]. Quach HT, et al. Eudesmane-Type Sesquiterpene Lactones Inhibit Nuclear Translocation of the Nuclear Factor κB Subunit RelB in Response to a Lymphotoxin β Stimulation. Biol Pharm Bull. 2017;40(10):1669-1677. [2]. Kang J, et al. Exposure to a combination of formaldehyde and DINP aggravated asthma-like pathology through oxidative stress and NF-κB activation. Toxicology. 2018 May 14;404-405:49-58.

Protocol

Cell experiment:

A549 cells transfectants stably expressing RelB WT and RelB (C144S) are preincubated with various concentrations of (-)-DHMEQ (1, 5, 10, 25, and 50 μM) for 1h and then incubated with or without LTβ (25 ng/mL) for 2 h in the presence or absence of (-)-DHMEQ.Cytoplasmic and nuclear extracts are analyzed by Western blotting[1].

参考文献:

[1]. Quach HT, et al. Eudesmane-Type Sesquiterpene Lactones Inhibit Nuclear Translocation of the Nuclear Factor κB Subunit RelB in Response to a Lymphotoxin β Stimulation. Biol Pharm Bull. 2017;40(10):1669-1677.
[2]. Kang J, et al. Exposure to a combination of formaldehyde and DINP aggravated asthma-like pathology through oxidative stress and NF-κB activation. Toxicology. 2018 May 14;404-405:49-58.