Tag: NRF2

Oltipraz is a Nrf2 Inhibitor

Multidrug resistance-associated proteins (Mrps) are ATP-dependent transporters involved in the efflux of a vast number of endogenous and exogenous chemicals. GSH is one of the liver’s main defenses against oxidative stress because of the conjugating, scavenging, and reducing capabilities of this molecule. GSH is essential to cellular defense against...

Brusatol (NSC 172924) is a Nrf2 Inhibitor

Keap1-Nrf2 is the major regulator of cytoprotective responses to electrophilic chemicals or reactive oxygen species (ROS).  Upregulation of Nrf2 inducing by inactivation of Keap1 is often observed in cancer cells. Aberrant activation of Nrf2 in cancer cells accelerates proliferation and metabolism. Meanwhile, Nrf2 is a transcription factor that regulates cellular...

PIK-75 is a Reversible DNA-PK and p110α Selective Inhibitor

PI3Ks catalyze the phosphorylation of the D-3 position of the inositol headgroup of phosphatidylinositol leading to the synthesis of second messengers PtdIns3P, PtdIns(3,4)P2, PtdIns(3,5)P2 and PtdIns(3,4,5)P3. The p110α and p110β are the main forms in insulin target tissues. Especially, p110α isoform (PIK3CA) plays the predominant role in insulin signaling....