UE01

Overview

UE01 is an orally active, selective small-molecule modulator targeting both ULK1/ERK1/2 . UE01 activates hULK1 with an EC 50 of 695.30 nM and a K D of 114.3 nM for ULK1 ; it inhibits hERK1 with an IC 50 of 179.90 nM and a K D of 114 nM for ERK1 ; it shows weak binding to ERK2 with a K D of 2.8 mM. UE01 induces the conformational transition of ULK1 from an inactive to an active state, enhances the phosphorylation of ULK1 Ser317 and mAtg13 Ser355, and reduces the phosphorylation of ULK1 Ser757. UE01 competitively occupies the ATP-binding pocket of ERK1 , inhibits ERK1 kinase activity, and reduces the activity of the ERK1/2 signaling pathway. UE01 induces complete autophagy flux and apoptosis , upregulates Atg5 , Atg7 , LC3-II/LC3-I , Bax , cytochrome C ( Cyt c ), Cleaved-Caspase 3 , Cleaved-PARP1 and E-cadherin , downregulates p62 , Bcl-2 , MMP-2 and MMP-9 , reduces the phosphorylation of Exo70 Ser250, and promotes the proteasome-dependent degradation of Cav-1, thereby inhibiting EMT-related phenotypes and extracellular matrix degradation. UE01 can be used in studies related to triple-negative breast cancer .

Application

Products | Products > Disease Areas > Cancer | Products > Disease Areas > Breast Cancer | Products > Disease Areas > Triple-Negative Breast Cancer | Products > Signaling Pathways > Autophagy | Products > Signaling Pathways > Stem Cell/Wnt | Products > Signaling Pathways > MAPK/ERK Pathway | Products > Signaling Pathways > Apoptosis | Products > Signaling Pathways > Metabolic Enzyme/Protease | Products > Research Areas > Cancer | Products > Research Areas > Cancer > Cancer Targeted Therapy | Products > Research Areas > Cancer > Cancer Stem Cells | Products > Research Areas > Cancer > Cancer Drug Resistance | Products > Research Areas > Cancer > Cancer Metabolism and Metastasis | Products > Signaling Pathways > Atg7 | Products > Signaling Pathways > p62 | Products > Signaling Pathways > Bcl-2 Family | Products > Signaling Pathways > MMP | Products > Signaling Pathways > ULK | Products > Signaling Pathways > ERK | Products > Signaling Pathways > Autophagy

Product Information

• Catalog No.: HY-184501
• CAS No.: 486440-74-8
• Molecular Formula: C18H13BrCl2N2O2
• Molecular Weight: 440.12
• Storage: Please store the product under the recommended conditions in the Certificate of Analysis.

Source

Original product source