KDM5-IN-1 (C09-1141-318)

KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC 50 of 15.1 nM.In VitroKDM5-IN-1 is found to potently inhibit KDM5B and KDM5C isoforms (IC 50 of 4.7 and 65.5 nM, respectively). It is significantly less potent against other KDM enzymes (1A, 2B, 3B, 4C, 5A, 6A, 7B), inhibiting KDM4C the strongest with an IC 50 of 1.9 μM. KDM5-IN-1 still displays more than 100-fold selectivity for KDM4C vs. KDM5A. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoWhen dosed orally in mice at 50 mg/kg twice a day, KDM5-IN-1 shows an unbound maximal plasma concentration C max >15-fold over its cell EC 50 , thereby providing a robust chemical probe for studying KDM5 biological functions in vivo . MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:IC50: 15.1 nM (KDM5),EC50: 0.34 μM (PC9 H3K4Me3). Specification: 0.99 Molecular Formula: C17H20N6O Molecular Weight: 324.38