SML1896

VH298

≥98% (HPLC)

• Sinónimos: (2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
• Fórmula empírica (notación de Hill): C₂₇H₃₃N₅O₄S
• Número de CAS: 2097381-85-4
• Peso molecular: 523.65
• Código UNSPSC: 12352200
• NACRES: NA.77

Propiedades

• ligand: VH298
• Nivel de calidad: 100
• Análisis: ≥98% (HPLC)
• formulario: powder
• idoneidad de la reacción: reagent type: ligand
• color: white to beige
• solubilidad: DMSO: 10 mg/mL, clear
• temp. de almacenamiento: −20°C

Descripción

Acciones bioquímicas o fisiológicas

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.

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable