1884220-36-3

1884220-36-3 structure

Name: SBI-0206965
Chemical Name: SBI-0206965
CAS Number: 1884220-36-3
Molecular Formula: C₂₁H₂₁BrN₄O₅
Molecular Weight: 489.319
Catalog: Signaling Pathways Autophagy ULK
Create Date: 2018-01-16 09:30:19
Modify Date: 2024-01-13 13:04:37
SBI-0206965 is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor with IC50 of 108 nM for ULK1 kinase activity and 711 nM for the highly related kinase ULK2 .IC50 value: 108nM/711 nMTarget: ULK1/ ULK2in vitro: 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.

Name	SBI-0206965
Synonyms	2-({5-Bromo-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl}oxy)-N-methylbenzamide Benzamide, 2-[[5-bromo-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl]oxy]-N-methyl-

Description	SBI-0206965 is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor with IC50 of 108 nM for ULK1 kinase activity and 711 nM for the highly related kinase ULK2 .IC50 value: 108nM/711 nMTarget: ULK1/ ULK2in vitro: 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.
Related Catalog	Signaling Pathways >> Autophagy >> ULK Research Areas >> Cancer
References	[1]. Egan DF, et al. Small Molecule Inhibition of the Autophagy Kinase ULK1 and Identification of ULK1 Substrates. Mol Cell. 2015 Jul 16;59(2):285-297.