TABLE 2

HIF-1α inhibitors and mechanisms of action

HIF-1α InhibitorMechanismReference
MagnololSuppresses PI3K-Akt-mTOR pathwayChen et al., 2013
SorafenibDecreases phosphorylation of mTOR and its downstream effectors p70S6K and 4E-BP1Liu et al., 2012
YC-1Suppresses the PI3K-Akt-mTOR-4E-BP pathwaySun et al., 2007
BEZ235Inhibits both PI3K and mTOR by interacting with their ATP-binding cleftsKarar et al., 2012
MeforminaInactivates mTOR by increasing the levels of REDD1Ben Sahra et al., 2011
DeferasiroaInactivates mTOR by increasing the levels of REDD1Ohyashiki et al., 2009
SP600125aInactivates mTOR by increasing the levels of REDD1Jin et al., 2009
TopotecanPrevents translation of HIF-1α mRNARapisarda et al., 2004
PX-4781) Decreases HIF-1α mRNA levels; 2) prevents HIF-1α translation; and 3) prevents HIF-1α deubiquitinationLee et al., 2011
  • a May actually increase HIF-1α levels.