SBI-0206965 is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor with IC₅₀s of 108 nM for ULK1 kinase and 711 nM for the highly related kinase ULK2 . IC50 & Target: IC50: 108 nM (ULK1 kinase), 711 nM (ULK2 kinase)^[2] In Vitro: SBI-0206965 (5-20 μM; 24 hours) induces apoptosis of A498 and ACHN cells during starvation^[1].
SBI-0206965 (5-20 μM; 24 hours) attenuates the phosphorylation of Ser108 of the AMPK β1 subunit and increases the levels of cleaved Caspase 8 and PARP, markers of apoptosis^[1]. In Vivo: SBI-0206965 (50 mg/kg; i.p.; once every 3 days for 37 days) inhibites tumour growth and induces apoptosis in A498 xenograft tumours^[1].