ULK Activator

UE01 is an orally active, selective small-molecule modulator targeting both ULK1/ERK1/2. UE01 activates hULK1 with an EC₅₀ of 695.30 nM and a K_D of 114.3 nM for ULK1; it inhibits hERK1 with an IC₅₀ 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.

BL-918 is an orally active UNC-51-like kinase 1 (ULK1) activator with an EC₅₀ of 24.14 nM. BL-918 exerts its cytoprotective autophagic effect by targeting ULK complex. BL-918 has the potential for Parkinson’s disease (PD) treatment.

LYN-1604 dihydrochloride is a potent UNC-51-like kinase 1 (ULK1) activator (EC₅₀=18.94 nM) for the research of triple negative breast cancer (TNBC).

LYN-1604 is a potent UNC-51-like kinase 1 (ULK1) activator (EC₅₀=18.94 nM) for the research of triple negative breast cancer (TNBC).

(Rac)-BL-918 is the racemate of BL-918. BL-918 is a potent activator of UNC-51-like kinase 1 (ULK1), inducing cytoprotective autophagy for Parkinson’s disease treatment.

LYN-1604 hydrochloride is a potent UNC-51-like kinase 1 (ULK1) activator (EC₅₀=18.94 nM) for the research of triple negative breast cancer (TNBC).

LYN-1604 (Standard) is the analytical standard of LYN-1604 (HY-101923). This product is intended for research and analytical applications. LYN-1604 is a potent UNC-51-like kinase 1 (ULK1) activator (EC₅₀=18.94 nM) for the research of triple negative breast cancer (TNBC).

LYN-1604 dihydrochloride (Standard) is the analytical standard of LYN-1604 dihydrochloride (HY-101923B). This product is intended for research and analytical applications. LYN-1604 dihydrochloride is a potent UNC-51-like kinase 1 (ULK1) activator (EC₅₀=18.94 nM) for the research of triple negative breast cancer (TNBC).