PROTAC MAGL degrader-1

PROTAC MAGL degrader-1 (JN-PROTAC) binds to purified MAGL protein via interactions with specific active site amino acid residues including Asn152, Leu176, and Arg240, and occupies the protein's core and cap region cavity^[1].
PROTAC MAGL degrader-1 (0.1-10 μM, 24 h) selectively degrades MAGL, shows a DC₅₀ of 60.28 nM and a D_max of roughly 95% in 528 glioblastoma stem cells, attains a DC₅₀ of 373.6 nM and a D_max of approximately 92.95% in X01 glioblastoma stem cells, and exhibits a typical hook effect at concentrations ≥ 50 μM^[1].
PROTAC MAGL degrader-1 (0.5 μM, 6-day incubation for proliferation assay; 14-day incubation for sphere formation assay) inhibits proliferation and sphere formation of X01 and 528 glioblastoma stem cells^[1].
PROTAC MAGL degrader-1 (0.1, 0.5 μM, 24 h) triggers apoptosis in glioblastoma stem cells in a concentration-dependent way and upregulates cleaved Caspase-3 as well as cleaved PARP^[1].
PROTAC MAGL degrader-1 (0.1-100 μM, 24 h) degrades endogenous MAGL protein in MDA-MB-231 human breast cancer cells and B16F10 mouse melanoma cells^[1].
PROTAC MAGL degrader-1 (0.5 μM, 24 h) markedly downregulates intracellular MAGL protein, and loses its degradation activity completely upon combined administration with 10 μM TAK-243 (HY-100487) or 10 μM MG-132 (HY-13259)^[1].


PROTAC MAGL degrader-1 (10 μM, 48 h) promotes the assembly of MAGL-JN-PROTAC-MDM2 ternary complex, competitively weakens the interaction between MDM2 and P53, and raises intracellular P53 levels within X01 cells in a dose-dependent fashion^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.