A potent, specific cell-active VHL E3 ubiquitin ligase inhibitor that inhibits VHL/HIF-α interaction with Kd of 90 nM in ITC assays; 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; induces HIF transcriptional activity and upregulates HIF-dependent response gene products, elicits a HIF-dependent hypoxic response in various cell lines.
CC-885 (CC 885, CC885) is a novel E3 ligase cereblon (CRBN) modulator with potent anti-tumour activity mediated through the degradation of GSPT1; The anti-tumour activity of CC-885 is mediated through the cereblon-dependent ubiquitination and degradation of the translation termination factor GSPT1; promotes both the in vivo and in vitro ubiquitination of GSPT1 by cereblon and decreases the protein half-life of GSPT1.
VH-032 (VHL ligand 1) is a VHL ligand for PROTAC and potent, small molecule inhibitor of the VHL/HIF-1α interaction with Kd of 185 nM.
VHL Ligand 4
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