KDM5-IN-1

KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC₅₀ of 15.1 nM. IC50 & Target: IC50: 15.1 nM (KDM5); EC50: 0.34 μM (PC9 H3K4Me3)^[1] In Vitro: KDM5-IN-1 is found to potently inhibit KDM5B and KDM5C isoforms (IC₅₀ 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 IC₅₀ of 1.9 μM. KDM5-IN-1 still displays more than 100-fold selectivity for KDM4C vs. KDM5A^[1]. In Vivo: When 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 EC₅₀, thereby providing a robust chemical probe for studying KDM5 biological functions in vivo^[1].