SML1896

VH298

≥98% (HPLC)

• Synonim(y): (2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
• Wzór empiryczny (zapis Hilla): C₂₇H₃₃N₅O₄S
• Numer CAS: 2097381-85-4
• Masa cząsteczkowa: 523.65
• Kod UNSPSC: 12352200

Właściwości

• Poziom jakości: 100
• Próba: ≥98% (HPLC)
• Postać: powder
• przydatność reakcji: reagent type: ligand
• kolor: white to beige
• rozpuszczalność: DMSO: 10 mg/mL, clear
• temp. przechowywania: −20°C

Opis

Działania biochem./fizjol.

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.

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable