MRT68921 is an inhibitor of ULK1 and ULK2 (IC₅₀s = 2.9 and 1.1 nM, respectively). Through its effects on ULK1, MRT68921 blocks autophagy in cells, driving the accumulation of stalled early autophagosomal structures.

≥98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

DMSO : 10 mg/mL, warmed

ULK1,ULK2

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.Petherick, K.J.,Conway, O.J.L.,Mpamhanga, C., et al. Pharmacological inhibition of ULK1 kinase blocks mammalian target of rapamycin (mTOR)-dependent autophagy. J. Biol. Chem. 290(18), 11376-11383 (2015).