AA-BR-157 is a metallothionein 2A (MT2A) PROTAC degrader, DC50 is 200 nM (MT2A overexpressed in MDA-MB-231 cells). AA-BR-157 increases intracellular zinc levels, downregulates DIAPH3, disrupts cytoskeleton remodeling, and reduces the migration and invasion abilities of cancer cells. AA-BR-157 can be used for research on triple-negative breast cancer and glioblastoma [1]. (Pink: MT2A ligand; Blue: VHL ligand; Black: linker ).
In Vitro, AA-BR-157 (0-30 μM; 24 h) (Compound 17) potently degrades overexpressed MT2A in MDA-MB-231 cells, with a DC50 of 200 nM and a Dmax of 90%[1]. AA-BR-157 (0-10 μM; 24 h) inhibits the migration of MDA-MB-231 and U-87 MG cells, as well as the invasion of MDA-MB-231 cells[1]. AA-BR-157 (10 μM; 12-24 h) increases intracellular zinc levels in MDA-MB-231 cells[1]. AA-BR-157 (0-10 μM; 24 h) downregulates the expression of DIAPH3 in MDA-MB-231 cells[1]. AA-BR-157 (10 μM; 24 h) induces a non-polarized, non-migratory cytoskeletal morphology in MDA-MB-231 cell[1].
References:
[1]. Racioppo B, et al. Chemoproteomics-Enabled De Novo Proteolysis Targeting Chimera Discovery Platform Identifies a Metallothionein Degrader to Probe Its Role in Cancer. J Am Chem Soc. 2025;147(9):7817-7828.
In Vitro, AA-BR-157 (0-30 μM; 24 h) (Compound 17) potently degrades overexpressed MT2A in MDA-MB-231 cells, with a DC50 of 200 nM and a Dmax of 90%[1]. AA-BR-157 (0-10 μM; 24 h) inhibits the migration of MDA-MB-231 and U-87 MG cells, as well as the invasion of MDA-MB-231 cells[1]. AA-BR-157 (10 μM; 12-24 h) increases intracellular zinc levels in MDA-MB-231 cells[1]. AA-BR-157 (0-10 μM; 24 h) downregulates the expression of DIAPH3 in MDA-MB-231 cells[1]. AA-BR-157 (10 μM; 24 h) induces a non-polarized, non-migratory cytoskeletal morphology in MDA-MB-231 cell[1].
References:
[1]. Racioppo B, et al. Chemoproteomics-Enabled De Novo Proteolysis Targeting Chimera Discovery Platform Identifies a Metallothionein Degrader to Probe Its Role in Cancer. J Am Chem Soc. 2025;147(9):7817-7828.