KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM.
IOX1 is the most potent broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases; IC50 for KDM4A/KDM3A is 0.6/0.1 uM.IC50 value: 0.6/0.1 uM(KDM4A/KDM3A) [1]Target: JmjC KDMs inhibitorIOX1 is the most potent against a representative panel of 2OG oxygenases, including non-JmjC 2OG oxygenases, with an in vitro IC50 value in the micromolar range. However, its efficacy in cells is about a hundred-fold lower (HeLa cells, KDM4A, IC50 = 86uM), possibly due to low cell permeability resulting from itspolar C-5 carboxyl group.
KDM2A/7A-IN-1 is a first-in-class, selective and cell-permeable inhibitor of histone lysine demethylases KDM2A/7A, with an IC50 of 0.16 μM for KDM2A, exhibits 75 fold selevtivity over other JmjC lysine demethylases, and is inactive on methyl transferases, and histone acetyl transferases[1].
SIRT2/6-IN-1 (Compound 5) is a SIRT6/SIRT2 inhibitor, with IC50s of 106 μM and 114 μM. SIRT2/6-IN-1 increases H3K9 acetylation, increases glucose uptake and reduces TNF-α secretion in cells[1].
LSD1-IN-13 hydrochloride (compound 7e) is an orally active and potent LSD1 inhibitor, with an IC50 of 24.43 nM. LSD1-IN-13 hydrochloride can activate CD86 expression, with an EC50 of 470 nM. LSD1-IN-13 hydrochloride induces differentiation of AML (acute myeloid leukemia) cell lines[1].