SML1896
VH298
≥98% (HPLC)
Synonyme(s) :
(2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
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About This Item
Formule empirique (notation de Hill):
C27H33N5O4S
Numéro CAS:
Poids moléculaire :
523.65
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77
Produits recommandés
ligand
VH298
Niveau de qualité
Pureté
≥98% (HPLC)
Forme
powder
Pertinence de la réaction
reagent type: ligand
Couleur
white to beige
Solubilité
DMSO: 10 mg/mL, clear
Température de stockage
−20°C
Catégories apparentées
Actions biochimiques/physiologiques
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.
Produit(s) apparenté(s)
Réf. du produit
Description
Tarif
Code de la classe de stockage
11 - Combustible Solids
Classe de danger pour l'eau (WGK)
WGK 3
Point d'éclair (°F)
Not applicable
Point d'éclair (°C)
Not applicable
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