TEPP-46

TEPP-46 (ML-265) is a potent and selective PKM2 activator. TEPP-46 activates tumor-specific PKM2 (EC₅₀ = 92 nM) by binding to the dimer-dimer interface between two subunits of PKM2 and inducing tetramerization, which is the most active form of the enzyme. In mice with A549 xenograft tumors, ML-265 displays good oral bioavailability with relatively low clearance, long half-life.