HIF-2a Translation Inhibitor 76

Biological Activity

HIF-2α-IN-4 is a potent inhibitor of hypoxia inducible factor-2α (HIF-2α) translation, with an IC50 of 5 μM. HIF-2α-IN-4 decreases both constitutive and hypoxia-induced HIF-2α protein expression. HIF-2α-IN-4 links its 5’UTR iron-responsive element to oxygen sensing[1]. HIF-2α-IN-4 (compound 76) (10 μM; 786-O cells) decreases HIF-2α mRNA translation in an mTOR-independent manner[1].HIF-2α-IN-4 decreases HIF-2α protein and HIF-2α target gene expression in normoxia and hypoxia[1].

References

[1]. Zimmer M, et al. Small-molecule inhibitors of HIF-2α translation link its 5’UTR iron-responsive element to oxygen sensing. Mol Cell. 2008;32(6):838-848.