SML1896

VH298

≥98% (HPLC)

• Synonym(e): (2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
• Empirische Formel (Hill-System): C₂₇H₃₃N₅O₄S
• CAS-Nummer: 2097381-85-4
• Molekulargewicht: 523.65
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• ligand: VH298
• Qualitätsniveau: 100
• Assay: ≥98% (HPLC)
• Form: powder
• Eignung der Reaktion: reagent type: ligand
• Farbe: white to beige
• Löslichkeit: DMSO: 10 mg/mL, clear
• Lagertemp.: −20°C

Beschreibung

Biochem./physiol. Wirkung

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.

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable