A cell-permeable, hydroxyquinoline HIF Prolyl Hydroxylase (PHD) inhibitor that displays an IC50 = 2 µM in a cell-based assay using a reporter produced by fusing HIF-1α oxygen degradable domain (ODD) to luciferase. This compound (5 µM) is shown to significantly stabilize HIF-1α in vitro and upregulate known HIF target genes, Epo and VEGF, in SH-SY5Y human neuroblastoma cell lines. It also exerts a neuroprotective effect (IC50 = 0.25 µM in an oxidative stress model using cortical neurons.
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Smirnova, N.A., et al. 2010. Chem. Biol.4, 380.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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Heat stress in ectotherms involves direct (e.g. protein damage) and/or indirect effects (temperature-induced hypoxia and ROS formation), which cause activation of the transcription factors (TF) heat shock factor 1 (HSF-1) and/or hypoxia-inducible factor 1 (HIF-1). The present study focused on
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