KDM5A-IN-1 is a potent, orally bioavailable pan- histone lysine demethylases 5 (KDM5) inhibitor with IC 50 s of 45 nM, 56 nM and 55 nM for KDM5A , KDM5B and KDM5C , respectively, and with an EC 50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B)
In Vivo
KDM5A-IN-1 (Compound 50, 5 mg/kg; oral administration; female CD-1 mice) treatment shows moderate clearance (28 mL/min/kg) in mice with good oral bioavailability (F% 34) and remarkably low plasma protein binding in mice (40%), with t 1/2 of 0.4 hours . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female CD-1 mice Dosage: 5 mg/kg Administration: Oral administration (Pharmacokinetic study) Result: Moderate clearance (28 mL/min/kg) in mice with good oral bioavailability (F% 34), and showed remarkably low plasma protein binding in mice (40%).
