JIB-04

JIB-04 is an epigenetic modifier that is a pan-selective inhibitor of Jumonji histone demethylase enzymes. It inhibits members of the family in the high nanomolar range with IC₅₀ values of 230, 340, 435, 445, 855 and 1100 nM for JARID1A, JMJD2E, JMJD2B, JMJD2A, JMJD3, and JMJD2C, respectively. It shows no activity against histone deacetylases and minimal effects against iron-containing enzymes methylcytosine dioxygenase TET1 and prolyl hydroxylases (Wang et al.; Easmon et al.).

CANCER RESEARCH

• Inhibits proliferation in a variety of human tumor cell lines (Easmon et al.).
• Selectively toxic to lung or prostate cancer cells in vitro, and not to normal cells of the same cell type or to normal control lines isolated from the same patient (Wang et al.).
• Reduces tumor burden and prolongs survival in a mouse model of breast cancer (Wang et al.).