Drug intelligence / Profile preview

STF-31 (faf94b)

Development stage
Discontinued
Modality
Small Molecules
01

Overview

STF-31 (also known as STF-III or Glucose Transporter Inhibitor III) is a small molecule inhibitor that targets glucose transporter 1 (GLUT1) and nicotinamide phosphoribosyltransferase (NAMPT). Originally identified through a high-throughput chemical synthetic lethal screen at Stanford University, STF-31 selectively induces necrotic cell death in von Hippel-Lindau (VHL)-deficient renal cell carcinoma (RCC) cells, which are highly dependent on GLUT1-mediated aerobic glycolysis (the Warburg effect) for survival. In addition to its direct binding and inhibition of GLUT1, STF-31 has been shown to inhibit NAMPT, a rate-limiting enzyme in NAD+ biosynthesis, which subsequently downregulates GLUT1 expression. STF-31 has been investigated preclinically for the treatment of renal cell carcinoma and other glycolysis-dependent cancers, as well as for the selective elimination of human pluripotent stem cells (hPSCs) from mixed cultures.

Other names
4-[[[[4-(1,1-dimethylethyl)phenyl]sulfonyl]amino]methyl]-N-3-pyridinyl-benzamide4-[[[[4-(tert-butyl)phenyl]sulfonyl]amino]methyl]-N-(pyridin-3-yl)benzamideGlucose Transporter Inhibitor IIISTF31STF-31STF 31
02

Targets

NAMPTGLUT1 (Glucose transporter 1)

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