MRT68921

MRT68921 is the most potent inhibitor of ULK1 and ULK2, with IC₅₀ values of 2.9 nM and 1.1 nM, respectively. IC50 & Target: IC50: 2.9 nM (ULK1), 1.1 nM(ULK2)^[1] In Vitro: ULK1, a serine/threonine protein kinase, is essential for the initial stages of autophagy. MRT68921 inhibits ULK1 and ULK2 in vitro and block autophagy in cells. MRT68921 is the most potent inhibitor of both ULK1 and ULK2, with greater than a 15-fold reduction in the IC₅₀ for ULK1 (2.9 nm) and greater than a 30-fold reduction for ULK2 (1.1 nm). Autophagy-inhibiting capacity of the compounds is specifically through ULK1. ULK1 inhibition results in accumulation of stalled early autophagosomal structures, indicating a role for ULK1 in the maturation of autophagosomes as well as initiation^[1].