A novel specific inhibitor of the Jumonji family of histone demethylases in vitro, in cancer cells and in tumors in vivo. IC50 = 230, 340, 435, 445, 855 and 1100 nM for JARID1A, JMJD2E, JMJD2B, JMJD2A, JMJD3 and JMJD2C respectively. Reduces tumor burden and prolongs life in a mouse model. Suppresses translation initiation and enhances mTOR inhibitor sensitivity. Inhibits the growth of temozolomide-resistant glioblastoma cells and crosses the blood brain barrier.
A recent study has shown that JIB-04 increases the expression of PD-L1 in SUM149-MA breast cancer cell lines. Increased PD-L1 expression in breast cancer cell lines renders them responsive to various therapies not just immune checkpoint blockade of PD-L1. Hence these results suggest that JIB-04 is a potential anti-cancer agent that can halt cancer progression and prevent resistance to therapies.
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