Signaling Pathway

Keap1-Nrf2

Keap1-Nrf2

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Keap1-Nrf2 is the major regulator of cytoprotective responses to oxidative and electrophilic stress. Kelch-like ECH-associated protein 1 is a protein that in humans is encoded by the Keap1 gene. Keap1 has been shown to interact with Nrf2, a master regulator of the antioxidant response, which is important for the amelioration of oxidative stress. Under quiescent conditions, Nrf2 is anchored in the cytoplasm through binding to Keap1, which, in turn, facilitates the ubiquitination and subsequent proteolysis of Nrf2. Such sequestration and further degradation of Nrf2 in the cytoplasm are mechanisms for the repressive effects of Keap1 on Nrf2. because Nrf2 activation leads to a coordinated antioxidant and anti-inflammatory response, and Keap1 represses Nrf2 activation, Keap1 has become a very attractive drug target.

Keap1-Nrf2 Inhibitors & Modulators (13)

Product Name Catalog No. Brief Description
Bardoxolone

HY-14909

Bardoxolone(RTA 402) is the lead molecule in Reata's portfolio of Antioxidant Inflammation Modulators (AIMs).

Bardoxolone methyl

HY-13324

Bardoxolone methyl(RTA 401; NSC 713200) is the lead molecule in Reata's portfolio of Antioxidant Inflammation Modulators (AIMs).

CDDO-EA

HY-12213

CDDO-EA(CDDO ethyl amide; RTA 405; TP319) is an activator of  Nrf2/ARE; Neuroprotective effect.

Curcumin

HY-N0005

Curcumin is a natural phenolic compound with impressive antioxidant properties.

Dimethyl fumarate

HY-17363

Dimethyl fumarate(DMF)  is a nuclear factor (erythroid-derived)-like 2 (Nrf2) pathway activator; induces upregulation of antioxidant gene expression.

Ezetimibe

HY-17376

Ezetimibe, a cholesterol-absorption inhibitor, reduces levels of low-density lipoprotein (LDL) cholesterol when added to statin treatment.

Ezetimibe D4

HY-17376S

Ezetimibe D4 is deuterium labeled Ezetimibe, which is a cholesterol-absorption inhibitor, reduces levels of low-density lipoprotein (LDL) cholesterol.

Gypenoside XVII

HY-N0553

Gypenoside XVII is a natural product.

Isoalantolactone

HY-N0780

Isoalantolactone, isolated from Inula spp.

NK-252

HY-19734

NK-252 is a Nrf2 activator, exhibits a greater Nrf2-activating potential than OPZ.

Nordihydroguaiaretic acid

HY-N0198

Nordihydroguaiaretic acid (NDGA) is a natural phenolic compound isolated from the creosote bush Larrea divaricata, which has anti-tumor activities both in vitro and in vivo.

RTA-408

HY-12212

RTA-408 is a synthetic triterpenoid that potently activates the antioxidative transcription factor Nrf2 and inhibits the proinflammatory transcription factor NF-κB.

Shogaol

HY-14616

6-shogaol, an active compound isolated from Ginger (Zingiber officinale Rosc), exhibits a variety of biological activities including anticancer, anti-inflammation, and anti-oxidation.