VH 298 is a potent, specific cell-active VHL E3 ubiquitin ligase inhibitor that inhibits VHL/HIF-α interaction with Kd of 90 nM in ITC assays.
VH 298 selectively engages VHL as its prime cellular target and is not toxic to cells, induces concentration- and time-dependent on-target specific accumulation of hydroxylated HIF-α in human cell lines.
VH 298 induces HIF transcriptional activity and upregulates HIF-dependent response gene products, elicits a HIF-dependent hypoxic response in various cell lines.
