GN44028

GN44028 is an inhibitor of HIF-1α transcriptional activity.¹ It reduces HIF-1α reporter gene expression in HeLa cervical cancer cells (IC₅₀ = 14 nM). GN44028 induces cytotoxicity in HCT116 colorectal, HepG2 hepatic, PC3 prostate, and HeLa cancer cells (IC₅₀s = 2.1, 3.7, 25.4, and 2.1 µM, respectively). It reduces the levels of VEGF, but not HIF-1α or HIF-1α-HIF-1β dimer levels, in HeLa cells when used at concentrations of 0.1 and 1 µM. In vivo, GN44028 (5 mg/kg twice per week), alone or in combination with 5-fluorouracil (Item. No. 14416), decreases tumor volume and the number of lung metastases and increases survival percentage in a CT26 murine colon cancer model.²

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1. Minegishi, H., Fukashiro, S., Ban, H.S., et al. Discovery of indenopyrazoles as a new class of hypoxia inducible factor (HIF)-1 inhibitors. ACS Med. Chem. Lett. 4(2), 297-301 (2013).

2. Liu, C., Zhang, W., Wang, J., et al. Tumor-associated macrophage-derived transforming growth factor-β promotes colorectal cancer progression through HIF1-TRIB3 signaling. Cancer Sci. 112(10), 4198-4207 (2021).