KDM5A-IN-1 is a potent and orally bioavailable inhibitor of pan-histone lysine demethylases 5 (IC50s: 45 nM, 56 nM, and 55 nM for KDM5A, KDM5B, and KDM5C) and (EC50: 960 nM for PC9 H3K4Me3). KDM5A-IN-1 is obviously less effective against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B).

KDM5A-IN-1 (5 mg/kg; p.o.; female CD-1 mice) treatment displays moderate clearance (28 mL/min/kg) in mice. It has good oral bioavailability (F% 34) and remarkably low plasma protein binding in mice (40%) (t1/2: 0.4 hours)[1].

1905481-36-8

C15H22N4O2

290.36

DMSO:50 mg/mL (172.20 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years