An inhibitor of ULK1 (IC50 = 108 nM) that is less effective against ULK2 (IC50 = 711 nM); suppresses autophagy induced by mTOR inhibition and blocks ULK1-dependent cell survival following nutrient deprivation

SBI-0206965 – 5 mg

Brand:
Cayman
CAS:
1884220-36-3
Storage:
-20
UN-No:
Non-Hazardous - /

ULK1 is a serine/threonine kinase that acts upstream of phosphatidylinositol 3-kinase (PI3K) to regulate the formation of autophagophores, the precursors of autophagosomes, in response to nutrient deprivation. It is activated by phosphorylation by AMPK and, in turn, phosphorylates and inhibits AMPK. SBI-0206965 is an inhibitor of ULK1 (IC50 = 108 nM) that is less effective against ULK2 (IC50 = 711 nM).{29597} It is selective for ULK1 and ULK2 over a panel of 456 additional kinases, showing activity against a few kinases in vitro but not in cells.{29597} SBI-0206965 suppresses autophagy induced by mTOR inhibition via AZD 8055 (Item No. 16978). It also blocks ULK1-dependent cell survival following nutrient deprivation.{29597}  

 

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Description

An inhibitor of ULK1 (IC50 = 108 nM) that is less effective against ULK2 (IC50 = 711 nM); suppresses autophagy induced by mTOR inhibition and blocks ULK1-dependent cell survival following nutrient deprivation

Formal name: 2-[[5-bromo-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl]oxy]-N-methyl-benzamide

Synonyms: 

Molecular weight: 489.3

CAS: 1884220-36-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Cell Biology|Endomembrane System & Vesicular Trafficking|Autophagy

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