VH298

VH298

Stock Code: 3575515
Manufacturer Part No: SML1896-25MG
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£605.89 (exc VAT) per 25MG
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Biochem/physiol Actions


VH298 is a cell-permeable small molecule that disrupts the interaction of VHL with Hypoxia-inducible factor HIF-α, stabilizing HIF-α and inducing a hypoxic response. Hypoxia-inducible factors (HIFs) are oxygen-sensitive transcription factors that regulate hypoxic signalling. They are regulated by oxygen-dependent prolyl hydroxylase domain (PHD) enzymes and polyubiquitination by the von Hippel–Lindau (VHL) Cullin RING E3 ubiquitin ligase complex. Unlike many PHD inhibitors, which have off-target effects, VH298 acts downstream of the PHD enzymes, inhibiting the VHL:HIF-α interaction. VH298 had a Kd of 90 nM. VH298 was shown to induce HIF transcriptional activity, to increase accumulation of HIF-α in HeLa cells and to stimulate erythropoietin production in RCC4 cells.


Packaging


5, 25 mg in glass bottle

Colourwhite to beige
Quality Level100
ManufacturerSIGMA-ALDRICH
Storage Temp.−20°C
SolubilityDMSO: 10 mg/mL, clear
Formpowder
Assay≥98% (HPLC)

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