VH-298 是一种高效的 VHL:HIF-α 相互作用抑制剂(Kd:80-90 nM)。它可用于PROTAC技术中。

VH-298 is a potent inhibitor of VHL that stabilizes HIF-α and elicits a hypoxic response via a different mechanism, that is the blockade of the VHL:HIF-α protein-protein interaction downstream of HIF-α hydroxylation by PHD enzymes.

VH298, a potent VHL inhibitor that stabilizes HIF-α and elicits a hypoxic response via a different mechanism, that is the blockade of the VHL:HIF-α protein-protein interaction downstream of HIF-α hydroxylation by PHD enzymes.?We show that VH298 engages with high affinity and specificity with VHL as its only major cellular target, leading to selective on-target accumulation of hydroxylated HIF-α in a concentration- and time-dependent fashion in different cell lines, with subsequent upregulation of HIF-target genes at both mRNA and protein levels.?VH298 represents a high-quality chemical probe of the HIF signalling cascade and an attractive starting point to the development of potential new therapeutics targeting hypoxia signalling.

2097381-85-4

C27H33N5O4S

523.65

DMSO:78.3mg/ml (149.53 Mm)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years