Biological Activity:

SBI-0206965 is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor. It inhibits ULK1 kinase with IC50 of 108 nM and the highly related kinase ULK2 with IC50 of 711 nM. It has very high selectivity, only inhibits 10 out of 456 kinases >95% when tested at 10 µM. SBI-0206965 suppressed ULK1-mediated phosphorylation events in cells, regulating autophagy and cell survival It can suppress autophagy induced by mTOR inhibition, prevent ULK1-dependent cell survival following nutrient deprivation. It greatly synergized with mechanistic target of rapamycin (mTOR) inhibitors to kill tumor cells, providing a strong rationale for their combined use in the clinic.

How to Use:

In vitro: SBI-0206965 was usually used at 10 µM final concentration in vitro.
In vivo: n/a

Reference:

• 1. Egan DF, et al. Small Molecule Inhibition of the Autophagy Kinase ULK1 and Identification of ULK1 Substrates. (2015) Mol Cell. 59(2):285-97.