jarid1a

GSK467 is a potent and selective inhibitor of KDM5 (JARID1)(Ki : 10 nM).

JIB-04 (NSC 693627) is a pan-selective Jumonji histone demethylase inhibitor.

CBB1007 trihydrochloride is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1). IC50 Value: 5.27 uM Target: hLSD1 CBB1007 efficiently can block LSD1-mediated demethylation of H3K4Me2 and H3K4Me (IC50 ≤ 5 μM) with no effect on H3K4Me3 and H3K9Me2, and LSD2 and JARID1A activities. Increases H3K4Me2 and H3K4Me contents (IC50 ≤ 5 μM), and causes activation of epigenetically suppressed CHRM4 M4-ArchR and SCN3A genes in F9 cells (IC50 ≤ 3.74 μM). CBB1007 was Shown to preferentially arrest the growth of pluripotent tumors with minimal effect on non-pluripotent cancer or normal somatic cells (IC50 ≥ 100 μM).

CBB1007 HCl is a cell-permeable amidino-guanidinium compound identified as a potent, reversible, and substrate-competitive inhibitor of LSD1 (IC50 = 5.27 μM for hLSD1). It effectively inhibits LSD1-mediated demethylation of H3K4Me2 and H3K4Me (IC50 ≤ 5 μM), without affecting H3K4Me3 and H3K9Me2 demethylation, nor the activities of LSD2 and JARID1A. Moreover, CBB1007 increases the levels of H3K4Me2 and H3K4Me (IC50 ≤ 5 μM) and activates epigenetically suppressed genes CHRM4 M4-ArchR and SCN3A in F9 cells (IC50 ≤ 3.74 μM). It preferentially inhibits the growth of pluripotent tumors with minimal impact on non-pluripotent cancer or normal somatic cells (IC50 ≥ 100 μM).

PBIT inhibits JARID1B histone demethylase (IC50 of about 3 μM). PBIT also inhibits JARID1A and JARID1C (IC50s of 6 μM and 4.9 μM, respectively). PBIT is a specific inhibitor of the Jumonji AT-rich Interactive Domain 1 (JARID1) enzymes .