SBI-0206965 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.
|Preparation method||Human embryonic kidney cells (HEK-293T) were transfected with wild-type (WT) or kinase inactive (KI) Myc-tagged ULK1 and wild-type Flag-tagged Vps34 (WT Vps34). 24 hours post-transfection, cells were treated with a panel of putative ULK1 competitive inhibitors in a dose response manner (1, 10, 50 μM). Cellular lysates were isolated after 1 hour of treatment and immunoblotted with the indicated antibodies.|
|Concentrations||1, 10, 50 μM|
|Incubation time||24 h|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||10 mM in DMSO|
SBI0206965, a novel inhibitor of Ulk1, suppresses non-small cell lung cancer cell growth by modulating both autophagy and apoptosis pathways.
Tang F, et al. Oncol Rep. 2017 Jun;37(6):3449-3458. PMID: 28498429.
Small Molecule Inhibition of the Autophagy Kinase ULK1 and Identification of ULK1 Substrates.
Egan DF, et al. Mol Cell. 2015 Jul 16;59(2):285-97. PMID: 26118643.
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