JBI-097 is a potent, dual LSD1/HDAC6 inhibitor with IC50 of 6/48 nM respectively, also inhibits HDAC8 (IC50=71 nM), does not inhibit other HDACs.
JBI-097 inhibited the proliferation of haematological cancers like acute myeloid leukaemia (AML), chronic myeloid leukaemia (CML), erythroleukaemia, and multiple myeloma with stronger potency with EC50 of 0.002-1.5 uM (MM1.S, EC50=2 nM).
JBI-097 also showed strong modulation of HDAC6 and LSD1 specific biomarkers, alpha-tubulin, CD86, CD11b, and GFi1b.
JBI-097 showed a stronger effect in erythroleukemia, multiple myeloma xenograft models, and in CT-26 syngeneic model.
JBI-097 also showed efficacy as monotherapy and additive or synergistic efficacy in combination with the standard of care or with immune checkpoint inhibitors.
