Biological Activity:MRT68921 is a potent, selective and dual autophagy kinase ULK1/2 inhibitor with IC50 of 2.9 nM and 1.1 nM, respectively. It can inhibit ULK in vitro and block autophagy in cells.By generating the drug-resistant M92T ULK1 mutant, MRT68921demostrates to specifically block autophagic flux through ULK1 inhibition and disrupt autophagosome maturation, not through AMPK-related kinase involvement.ULK1 inhibition results in accumulation of stalled early autophagosomal structures, indicating a role for ULK1 in the maturation of autophagosomes as well as initiation.How to Use:In vitro:MRT68921 was usually used at 1 µM final concentration in vitro.In vivo: n/aReference:

• 1.Petherick KJ, et al. Pharmacological inhibition of ULK1 kinase blocks mammalian target of rapamycin (mTOR)-dependent autophagy. (2015) J Biol Chem. 290(18):11376-83.

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