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Biological Activity:

GN44028 is potent and selective HIF-1α inhibitor with IC50 ~14 nM. It inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization in nuclei under the hypoxic conditions. This suggests that GN44028 probably affected the transcriptional pathway induced by the HIF-1α/HIF-1β heterodimer.

How to Use:

In vitro: GN44028 was used at 1-10 µM in vitro and cellular assays.
In vivo: n/a

Reference:

• 1. Minegishi H, et al. Discovery of Indenopyrazoles as a New Class of Hypoxia Inducible Factor (HIF)-1 Inhibitors. (2013) ACS Med Chem Lett. 4(2):297-301.