GN44028

A cell-permeable indenopyrazole based compound that potently suppresses hypoxia-induced HIF-1α transcription (IC₅₀ = 14 nM in HRE-Luc HeLa cells) and VEGF-expression. Shown to effectively induce growth arrest in several cancer cells (IC₅₀ = 2.1, 3.7 & 1.8 µM for HCT116, HepG2 & HeLa cells), although with reduced efficiency in PC3 (IC₅₀ = 25.4 µM). Does neither affect HIF-1α protein accumulation nor HIF-1α/HIF-1β heterodimer complex formation. Suggested to act via impairing HIF-1α/HIF-1β heterodimer-induced transcriptional pathway.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Cell permeable: yes

Primary Target
HIF-1α

Reversible: yes

Secondary Target
VEGF

Target IC₅₀: 14 nM in HRE-Luc HeLa cells

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Minegishi, H., et al. 2013. ACS Med. Chem. Lett.4, 297.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)