NSC-134754

NSC-134754 is a small molecule inhibitor of Hypoxia-Inducible Factor 1 (HIF-1) identified through the National Cancer Institute (NCI) Developmental Therapeutics Program. It acts by reducing HIF-1α protein levels and transcriptional activity, although it does not appear to affect HIF-1α mRNA expression. In preclinical research, NSC-134754 has demonstrated the ability to inhibit vasculogenesis and tumor recurrence following radiotherapy. This effect is mediated by preventing the recruitment of bone marrow-derived pro-angiogenic cells, such as CD11b+ myelomonocytes, to the tumor site in response to radiation-induced hypoxia. It has been primarily studied in models of glioblastoma and head and neck squamous cell carcinoma.