中文名称:VH298

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。

CAS No:2097381-85-4

产品描述：
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.

体外活性：

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.

分子式：
C27H30N5O4S

分子量：
523.65

参考文献：
[1]Frost J, et al. Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition. Nat Commun. 2016 Nov 4;7:13312.

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

Note：
For research use only .