KDM5-IN-48 is a novel, potent, selective and orally bioavailable KDM5 inhibitor (IC50 o=15.1 nM). KDM5-IN-48 has improved cell potency (PC9 H3K4Me3 EC50=0.34μM). Furthermore, KDM5-IN-48 maintained suitable physiochemical properties and displayed an excellent pharmacokinetic (PK) profile in mice. When dosed orally in mice at 50mg/kg twice a day (BID), KDM5-IN-48 showed an unbound maximal plasma concentration (Cmax) >15-fold over its cell EC50, thereby providing a robust chemical probe for studying KDM5 biological functions in vivo.
纯度:≥98%
CAS:1628210-26-3