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
• Formule empirique (notation de Hill): C₂₇H₃₃N₅O₄S
• Numéro CAS: 2097381-85-4
• Poids moléculaire : 523.65
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• ligand: VH298
• Niveau de qualité: 100
• 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

Description

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.

Informations sur la sécurité

• 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